ライフサイエンスコーパス: piperidine

1 omega-unsaturated N-sulfanilamide to furnish piperidines.

2 ve as useful building blocks for substituted piperidines.

3 uilding block for the synthesis of annulated piperidines.

4 zones to afford substituted pyrrolidines and piperidines.

5 es, pyrimidines, quinolines, thiophenes, and piperidines.

6 ctical procedure for the synthesis of chiral piperidines.

7 d for the synthesis of functionalized chiral piperidines.

8 for the azetidines than for the matched-pair piperidines.

9 d diazoketones for the rapid construction of piperidines.

10 ted aldehydes afford trans-2,4-disubstituted piperidines.

11 drobase intermediates afforded 4-substituted piperidines.

12 yl aziridines, azetidines, pyrrolidines, and piperidines.

13 ered as elongated analogues of 3-substituted piperidines.

14 ient entry to this class of pyrrolidines and piperidines.

15 tial activities of the above piperazines and piperidines.

16 cluding pyridines, pyrimidines, indoles, and piperidines.

17 ts in a variety of 2-substituted 1-(methyl-d)piperidines.

18 mmonium persulfate and 2,2,6,6-tetramethyl-1-piperidine 1-oxyl (TEMPO), is described.

19 ting materials, the transformations into the piperidines 1-deoxygalactonorjirimycin (DGJ) and 4-epi-f

20 ituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine (1) class of opioid receptor antagonists, pro

21 2573X (4-(2-methoxyphenylcarbamoyloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester).

22 ing solids (HYPSOs) with 2,2,6,6-tetramethyl-piperidine-1-oxyl radicals incorporated in a mesostructu

23 ning the nitroxide probe 2,2,6,6-tetramethyl-piperidine-1-oxyl-4-amino-4-carboxylic acid substituted

24 In 2,2,6,6-tetramethyl-piperidine-1-oxyl-4-amino-4-carboxylic acid, the probe i

25 molecule [5-(3,4-dichlorophenyl)furan-2-yl]-piperidine-1-ylmethanethione (DFPM) has previously been

26 molecule [5-(3,4-dichlorophenyl)furan-2-yl]-piperidine-1-ylmethanethione (DFPM) that rapidly downreg

27 -molecule [5-(3,4-dichlorophenyl)furan-2-yl]-piperidine-1-ylmethanethione (DFPM) that triggers rapid

28 3-ylm ethyl)-2-oxoethyl]spiro[1H-indene-1,4'-piperidine]-1'-carboxamide) in DA amacrine cells and the

29 e; 2 mum) and M3- (diphenyl-acetoxy-N-methyl-piperidine; 100 nm) receptor blockers, but not by a nico

30 Two compounds, which contain a piperidine (14) or an isoindoline (17) pendant, retained

31 alpha-Piperidine 19v (SC-78080/SD-2590) was selected for devel

32 late) with the cyclic diamine 2-(aminomethyl)piperidine (2-ampd) produces an adsorbent that is capabl

33 reduced with high stereoselectivity to give piperidines, (2) participate in [3 + 2] dipolar cycloadd

34 N-substituted prolinamides or N-substituted piperidine-2-carboxamides via a metal-free decarboxylati

35 nsus motif of D-pThr-Pip-Nal (where Pip is L-piperidine-2-carboxylic acid and Nal is L-2-naphthylalan

36 s of benzoxazolone carboxamides resulting in piperidine 22m, where we demonstrated target engagement

37 ituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines (2a,b) are opioid receptor antagonists where

38 In a modified Folts model in dog, both piperidine 3 and azetidine 13 dose-dependently induced i

39 ]-1-[3-(2,3,5-trifluorophenyl) -prop-2-ynyl]-piperidine-3-carboxylic acid) (RPR) induces a pronounced

40 ]-1-[3-(2,3,5-trifluorophenyl )-prop-2-ynyl]-piperidine-3-carboxylic acid] (RPR) slows deactivation a

41 By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexyla

42 On the basis of the 6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] framework, a series

43 eveloped (S)-3-(2'-fluoro-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran]-1-yl)-2-( 2-fluorobe

44 The synthesis of 4',6'-dihydrospiro[piperidine-4,5'-pyrazolo[3,4-c]pyridin]-7'(2'H)-one-base

45 el chemical series based on the dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.

46 Herein we show that dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran)-derived compounds ar

47 igh-affinity 3-(2'-fluoro-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran]-1-yl)-2-(2-ha lobenz

48 s, built on the structure of 1-(pyridin-4-yl)piperidine-4-carboxamide, are described.

49 ypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidi n-4-yl)piperidine-4-carboxamide] and WEE1 inhibitor AZD1775 [2-

50 d 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as potent and orally bioavaila

51 (2,4-diaminopteridin-6-ylmethylamino)benzoyl]piperidine-4-carboxylate (1) led to the synthesis of a f

52 tive desymmetrization of achiral N,N-dialkyl piperidine-4-carboxylates to give products with two or t

53 y neurosteroids, and the agonist activity of piperidine-4-sulfonic acid (P4S) were determined.

54 airs of orthosteric (GABA, beta-alanine, and piperidine-4-sulfonic acid) and/or allosteric agents (pr

55 o) and rectification with a partial agonist, piperidine-4-sulfonic acid, and a gating-impaired mutati

56 7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol and piperidine-4-sulfonic acid, we examined BDZ modulation u

57 ingle atom to tetrahydropyran 3 and N-acetyl piperidine 5.

58 ometric dynamic resolution of 2-lithio-N-Boc-piperidine (7) have been investigated.

59 Compared to amantadine, spiro-piperidine 9 (1) induces a more homogeneous conformation

60 phenolic oxygen (gamma-attack), whereas for piperidine a hydrogen bond between the hydrogen on the i

61 On the other hand, in the presence of piperidine, a significant reduction in the ion currents

62 Starting from 3-hydroxy piperidines, a novel transition-metal-free strategy to 5

63 ontrast, the linker composed of squarate and piperidine accesses different conformations in their res

64 densation ( approximately 40 mM, rt, CH2Cl2, piperidine/AcOH/molecular sieves) of a dihydrodipyrrin-c

65 lasubine I, (+)-lasubine II, and substituted piperidine alkaloid (+)-241-D.

66 ine (+)-myrtine and cis-2,4,6-trisubstituted piperidine alkaloid (+)-241D are reported here.

67 The synthesis of the piperidine alkaloid (-)-pelletierine was successfully un

68 etic route to tricyclic analogues of the bis(piperidine) alkaloid xestoproxamine C are presented.

69 The synthesis of the piperidine alkaloids (+)-241D, (-)-epimyrtine, and (-)-l

70 es were estimated for plant genera producing piperidine alkaloids (horsetail), furanocoumarins (parsl

71 40, 41, 48, and 49, with C-28 piperazine or piperidine amide substitutions, increased the activity b

72 4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaff

73 phatic substituents directly attached to the piperidine amine (i.e., lacking the spacer) have decreas

74 s of 2-substituted 2-phenylpyrrolidines and -piperidines, an important class of pharmaceutically rele

75 This quinolyl-piperazinyl piperidine analogue displayed potent, selective 5-HT(1A)

76 the morpholines, unlike the pyrrolidine and piperidine analogues, have been found to be brain penetr

77 he initial indication of cancer, while alpha-piperidine and alpha-tetrahydropyranyl hydroxamates 19w

78 alpha-Sulfone-alpha-piperidine and alpha-tetrahydropyranyl hydroxamates were

79 Computational studies of the reaction of piperidine and dimethylamine with the same aryl halides

80 n of (2R,R(S))-2-allyl-(N-tert-butylsulfinyl)piperidine and its enantiomer is detailed.

81 more, pirenzepine, diphenyl-acetoxy-N-methyl-piperidine and mecamylamine had no measurable effect on

82 ynthesis of fluoroaminosulfones derived from piperidine and nucleic bases followed by the study of th

83 pproach to the synthesis of polyhydroxylated piperidine and pyrrolidine peptidomimetics is described.

84 is(3,4-dimethoxyphenyl)ethane via two bases, piperidine and pyrrolidine, has been computationally inv

85 available enzymes, which revealed the sugar-piperidine and sugar-pyran hybrids as potent and selecti

86 cyclization reactions to afford a variety of piperidine and tetrahydroisoquinoline structures.

87 Variation of the linker group between the piperidine and the lipophilic substituent identified 4-a

88 to provide the corresponding functionalized piperidines and pyrrolidines.

89 line, tetrahydroisoquinoline, benzimidazole, piperidine) and alkylene spacers (2 to 10 methylene grou

90 N-protected aziridines, pyrrolidines, piperidines, and azepanes bearing aromatic, heteroaromat

91 2,2-disubstituted azetidines, pyrrolidines, piperidines, and azepanes bearing ester and diverse aryl

92 disubstituted alkenes afforded pyrrolidines, piperidines, and azepanes in high yields and high enanti

93 ormed to access functionalized pyrrolidines, piperidines, and azepanes with a general preference for

94 icyclic building blocks, including oxetanes, piperidines, and azetidines, from their parent ketones.

95 lecule scaffold for NPFF1,2-R, the guanidino-piperidines, and SAR studies resulting in the discovery

96 on of a variety of substituted pyrrolidines, piperidines, and tetrahydroisoquinolines through alkylat

97 ration of 2,6-cis or 2,6-trans disubstituted piperidines are described, through intramolecular reacti

98 Piperidines are prevalent in natural products and pharma

99 voids the use of hazardous components (using piperidine as a base and dichloromethane (DCM) and N,N-d

100 ve methylenes, and alpha-azido ketones using piperidine as a catalyst in the aqueous medium through a

101 orono-Mannich reaction using benzylamine and piperidine as representative examples of primary and sec

102 ree homoallylamine affording the deprotected piperidine as single cis diastereomer.

103 extends the scope of saturated azacycles to piperidines, azepane, and tetrahydroisoquinoline that ar

104 lude ethyl amines, azetidines, pyrrolidines, piperidines, azepanes, indolines and tetrahydroisoquinol

105 t N-protected methyl-substituted spirocyclic piperidine-azetidine (2,7-diazaspiro[3.5]nonane) and spi

106 identification of a series of pyrrolidine or piperidine based full agonists and attempted optimizatio

107 any inhibitory activity of IdeS, but several piperidine-based analogues were identified as inhibitors

108 loped a novel series of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and selec

109 tabolites by attaching high proton affinity, piperidine-based chemical tags to each carboxylic acid g

110 )-catalyzed rearrangement of piperidones and piperidines bearing a spirocyclopropane ring was develop

111 itations of the reaction were explored, with piperidines bearing multiple substitution patterns provi

112 represent a new class of lead compounds with piperidine, benzothiophene, and indole scaffolds to inhi

113 te a twisted conformation about the pyridine-piperidine bond of 9 by small-molecule X-ray crystallogr

114 A synthetic strategy to fused bicyclic piperidines-building blocks for medicinal chemistry-is d

115 (e.g., carboxamide, alkylamine, piperazine, piperidine, but not sulfonamide) were well tolerated in

116 ral route to cis- or trans-2,6-disubstituted piperidines by lithium aluminum hydride reduction of the

117 Piperidine carboxamide 1 was identified as a novel inhib

118 -[4-chlorophenyl]-1-[3-(2-furanyl)benzoyl]-3-piperidine carboxamide) and/or Fas-activating antibody i

119 Here we report a class of piperidine carboxamides (PIPCs) as potent, noncovalent a

120 g sizes (azetidine carboxylic acid, Aze, and piperidine carboxylic acid, Pip) to produce different tr

121 The rate law for styrene hydroamination with piperidine catalyzed by [Sr{N(SiMe(3))(2)}(2)](2) was de

122 quiv of 1,3-dicarbonyl compounds involving a piperidine-catalyzed ABB' three-component domino process

123 A Veratrum piperidine chiron was prepared over 11 steps (7.9% yield

124 ecule allosteric ligand from the piperazinyl-piperidine class, also known as VUF11211 [(S)-5-chloro-6

125 in the isomerization step, whereas the CuCl-piperidine complex (formed during the cross coupling) ma

126 the study was focused on oligo(piperidinone-piperidine) compounds I.

127 X-ray data of a variety of published N-acyl-piperidine-containing compounds further indicates that t

128 in the preparation and biological studies of piperidine-containing structures.

129 r the assembly of the stereochemically dense piperidine core of 205B is noteworthy, as this method en

130 hetic strategies focused on constructing the piperidine core of the calyciphylline B-type framework v

131 Only in the case of 2,6-disubstituted piperidines, could the "quaternization-hydride reduction

132 (DOTA-AR), and DOTA-(4-amino-1-carboxymethyl-piperidine)-[D-Phe(6), Sta(13)]-BN(6-14)NH2 (DOTA-RM2).

133 (68)Ga-labeled DOTA-4-amino-1-carboxymethyl-piperidine-D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 ((6

134 (68)Ga-labeled DOTA-4-amino-1-carboxymethyl-piperidine-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 ((6

135 Pyrrolidines, tetrahydropyridines, and piperidines decorated with various aromatics and substit

136 rward synthesis of a natural trihydroxylated piperidine demonstrates the utility of these unsaturated

137 pproach was developed, and 3,4-disubstituted piperidine derivative S-28 was identified as a lead comp

138 The rational combination of dicationic piperidine-derivative molecules as organic structure dir

139 entify a pregnanol derivative and a class of piperidine derivatives that differentially modulate gene

140 C-H arylation reaction of highly substituted piperidine derivatives with electron-deficient cyano(het

141 methodology that provides highly substituted piperidine derivatives with regiochemistry selectively t

142 ynthesis of polysubstituted cyclopentane and piperidine derivatives.

143 Piperidine-derived analogues showing minimal microsomal

144 ype addition of an indole ester dianion to a piperidine-derived nitrosoalkene to form the C15, C16 bo

145 4-Substituted piperidine-derived trisubstituted ureas are reported as

146 e surface with copper nanoparticles-ammonium piperidine dithiocarbamate-mutiwalled carbon nanotubes a

147 ving the 3-hydroxyphenyl group locked in the piperidine equatorial orientation had potencies equal to

148 mpounds, and identified a group of phenethyl piperidines (exemplified by LD7), which reduces the accu

149 Substitution of a piperidine for the piperazine of sabiporide followed by

150 The utility of this piperidine forming strategy as a synthetic tool that mak

151 synthesis of densely substituted, oxygenated piperidines from two classes of tetrahydropyridines with

152 2-(2-propynyl)pyrrolidine and 2-(2-propynyl)piperidine gave 2-(9-phenanthylmethyl)pyrrolidines and 2

153 and docking studies with 1 indicate that the piperidine group could be functionalized at the 4-positi

154 structure-guided derivatives with an altered piperidine group, predicted to improve binding, show enh

155 free synthetic strategy for the synthesis of piperidines has been explored.

156 -n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)piperidine HCl) and 77-LH-28-1 (1-(3-(4-butyl-1-piperidi

157 n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine hydrogen chloride), TBPB (1-[1'-(2-methylbenz

158 vel, easily accessible 4-(1- and 2-adamantyl)piperidines, identified as dual binders of the wild-type

159 ty afforded corresponding 5C-dihydroxymethyl piperidine iminosugars 2a-c.

160 ophenyl phosphate triester (Paraxon, 1) with piperidine in ionic liquids (ILs), three conventional or

161 proline, nitrobenzaldehyde, pyrrolidine, and piperidine in two to four operational steps without chro

162 ent method to construct 2,3,6-trisubstituted piperidines in a substituent-independent fashion.

163 (S(S),R)-N-tert-butanesulfinyl-2-substituted piperidines in excellent yield (98%) and with high diast

164 (S(S),S)-N-tert-butanesulfinyl-2-substituted piperidines in good yield (98%) and with high diastereos

165 A range of enantiopure polyhydroxylated piperidines, including (2R,3S,4R)-dihydroxypipecolic aci

166 An efficient synthesis of key chiral piperidine intermediate 1 suitable for large-scale prepa

167 2-Substituted N-acyl-piperidine is a widespread and important structural moti

168 The piperidine is studied as a linker, functionalized with a

169 g asymmetric deprotonation trapping of N-Boc piperidine is successfully realized using s-BuLi and a (

170 ethodology to the formation of 2-substituted piperidines is also illustrated.

171 id and a Bronsted acid to efficiently afford piperidines is described.

172 e to access 2-unsubstituted pyrrolidines and piperidines is presented.

173 A novel approach to 2,4,5-trisubstituted piperidines is reported, involving the 6-exo cyclization

174 of pharmaceutically important N-(hetero)aryl piperidines is reported.

175 termining step in the stereomutation of such piperidines is the piperidine ring flip and not nitrogen

176 ivity between the cis- and trans-substituted piperidine isomers.

177 a 2-lithiated pyrrolidine than a 2-lithiated piperidine; low yields for the lithiation-substitution o

178 oumarin scaffold to 1,3- and 1,4-substituted piperidine moieties, thus modulating the basicity to imp

179 y synthesized peptide analogues containing a piperidine moiety as a replacement of a glycine residue

180 urine-based Hsp90 inhibitor 28a containing a piperidine moiety at the purine N9 position.

181 ydrophobic pocket, with the outward pointing piperidine moiety being the most flexible.

182 Potency was enhanced by replacing the piperidine moiety by N,N-dibutyl, N,N-diisobutyl, or N,N

183 ubstrate access channel antechamber with its piperidine moiety forming a charge-stabilized hydrogen b

184 The protonated piperidine moiety of thioridazine forms a charge-stabili

185 as significantly increased by exchanging the piperidine moiety with either N,N-dipropyl, N,N-diisopro

186 h an electron-withdrawing substituent in the piperidine moiety, such as R,S-7c, retained the Gram-pos

187 l drug candidate containing a trisubstituted piperidine moiety.

188 from acetophenone or phenylacetaldehyde and piperidine, morpholine, or pyrrolidine were located usin

189 om cyclic amines and diamines (pyrrolidines, piperidines, morpholines, and piperazines) by the cumylo

190 I3Kdelta inhibitor bearing a benzimidazolone-piperidine motif was found to be poorly tolerated in dog

191 b was directly conjugated to Dha through its piperidine motif, and its antibody-mediated intracellula

192 of this method are well-suited for appending piperidine motifs to natural product and complex molecul

193 found that a cyclohexylmethyl residue at the piperidine N-atom instead of a benzyl moiety led to incr

194 conditions and employ 2,2,6,6-tetramethyl-1-piperidine N-oxyl (TEMPO) and 4-acetamido-TEMPO (ACT) as

195 ion reactions (TEMPO = 2,2,6,6-tetramethyl-1-piperidine N-oxyl).

196 this study, key SAR was established for the piperidine N-substituent and for the congeners of the 1,

197 urs from the C-H bonds that are alpha to the piperidine nitrogen (alpha-C-H bonds).

198 2, protonation or Mg(2+) complexation of the piperidine nitrogen removes the intramolecular hydrogen

199 utions at the indazole 5-position and at the piperidine-nitrogen to obtain potent ATP-competitive GSK

200 nds are synthetically accessible, with rigid piperidine or quinuclidine analogues of TPMA(NMe2) posse

201 basis of known M(3) antagonists comprising a piperidine or quinuclidine unit attached to a biphenyl c

202 n hydride to afford the 2,4,5-trisubstituted piperidine or undergo a second 5-endo cyclization onto t

203 either reduced in situ to the corresponding piperidine or used to achieve the stereoselective constr

204 Cyclization to form pyrrolidines, piperidines, or morpholines results in a preorganization

205 (N-MPIPZ) < 4-piperidinemethanol (4-PIPDM) ~ piperidine (PIPD) < pyrrolidine (PYR).

206 tera)cyclobutyl)azetidine-based isosteres of piperidine, piperazine, and morpholine were designed and

207 relationships, and inhibitory activities of piperidine/piperazine carbamates against members of the

208 Piperidine/piperazine carbamates show excellent in vivo

209 re both inhibited by carbamates bearing an N-piperidine/piperazine group.

210 Modifications to the piperidine/piperazine ring ablated inhibitory activity,

211 r aryloxybenzyl moiety, respectively, on the piperidine/piperazine ring.

212 nantioenriched N-Boc-2-phenylpyrrolidine or -piperidine (prepared by asymmetric Negishi arylation or

213 ssful and gave the allylated pyrrolidine and piperidine products with good enantioselectivity, althou

214 e substituted pyridine, dihydropyridine, and piperidine products.

215 ydroxyphenyl)-beta-methyl-4-(phenylmethyl)-1-piperidine propranol], and hippocampal small interfering

216 ydroxyphenyl)-beta-methyl-4-(phenylmethyl)-1-piperidine propranol].

217 More rigid piperidines provided the highest selectivity of the reac

218 active co-potentiators of pyrazoloquinoline, piperidine-pyridoindole, tetrahydroquinoline and phenyla

219 building blocks, including those containing piperidine, pyrrole, azetidine, tetrahydropyran, and oxe

220 (2,7-diazaspiro[3.5]nonane) and spirocyclic piperidine-pyrrolidine (2,8-diazaspiro[4.5]decane) ring

221 ed for the synthesis of 1-methyl spirocyclic piperidine-pyrrolidine with a classical resolution of th

222 on of hydroxy-substituted alkenylamines into piperidines, pyrrolidines, and furans.

223 pyrazole-4-arylsulfonyl-piperazine and spiro-piperidine-quinazolinone classes were identified with up

224 talysts including pyrimidines, N-substituted piperidines, quinolines, indoles, N-substituted imidazol

225 hit-finding approach, the 3,5-disubstituted piperidine (rac)-5 was discovered by HTS using a enzymat

226 l-stabilized radical gives the corresponding piperidine radical as a single diastereoisomer that may

227 clizations, furnishing either pyrrolidine or piperidine, respectively.

228 deprotonation of N-Boc-pyrrolidine and N-Boc-piperidine, respectively.

229 ethyl)pyrrolidines and 2-(9-phenanthylmethyl)piperidines, respectively.

230 kinetic resolution of various disubstituted piperidines revealed a strong preference for the acylati

231 Bicyclic-substituted piperidine ring derivatives of naphthalene antagonist 1,

232 he stereomutation of such piperidines is the piperidine ring flip and not nitrogen inversion or rotat

233 A 2,4,6-trisubstitited piperidine ring forms the core of the quinolizidine segm

234 membered bicyclic aryl rings attached to the piperidine ring had a marked impact on these effects.

235 ain between the arene and tosyl group on the piperidine ring is proposed to rationalize the greater s

236 ectrostatic interaction between the ORG27569 piperidine ring nitrogen and K3.28(192) that is importan

237 y step was employed to construct the central piperidine ring of the iminosugar and the C-glycosidic s

238 l ether substituent on the 5-position of the piperidine ring provided ultrapotent inhibitor 38 (DH376

239 ands, cyTPA and 1-isocyTPQA, which feature a piperidine ring that provides a structurally rigid backb

240 e and (ii) introduction of a fluorine in the piperidine ring to reduce its basicity, resulting in att

241 7 indicated that the benzylated six-membered piperidine ring was disordered and exposed to solvent.

242 A C2-symmetric piperidine ring was incorporated in the ligand as the ni

243 nteractions to control the conformation of a piperidine ring.

244 rrect relative stereochemistry about the bis(piperidine) ring system.

245 complex noviose sugar with readily available piperidine rings resulted in approximately 100 fold incr

246 precedented level of substitution to provide piperidine rings with adjacent tetrasubstituted carbon a

247 oducts containing only fused pyrrolidine and piperidine rings.

248 ediates, however, in the oligo(pyrrolidinone-piperidine)s H syntheses were vulnerable to epimerizatio

249 ructural modifications on the trisubstituted piperidine scaffold of 11i yielded compounds with high C

250 linkers derived from chiral pyrrolidine and piperidine scaffolds.

251 The piperidine segment was coupled in a B-alkyl Suzuki react

252 luding reconstruction of the benzimidazolone-piperidine selectivity motif.

253 n spirocyclohexane-substituted nitroxides of piperidine series and showed 1.3-3.14 times lower reduct

254 e base used [MeONa or a silica gel-supported piperidine (SiO(2)-Pip)], and the main electrolysis para

255 le C-H functionalization of three unreactive piperidine sp(3) carbons.

256 ioselective preparation of 2,6-disubstituted piperidines starting from easily accessible pro-chiral k

257 The program described herein varied a 3-piperidine substituent and incorporated 4-thiazole subst

258 ablish pyridine-substituted pyrrolidines and piperidines, successful homologation of pyridine-4-carbo

259 N-Linked amino piperidines, such as 7a, generally show potent antibacte

260 lar cyclization process of a N-Boc-protected piperidine sulfone.

261 cal shift difference in 2-methyl-1-(methyl-d)piperidine supports a long-lived nuclear spin state.

262 lizing a functionalized pyridine moiety as a piperidine surrogate.

263 d to the diastereomeric 2,4,5-trisubstituted piperidines syn-5m, -5n, -5o and anti-5m, -5n, -5o.

264 limitations of the carbamate annulation for piperidine synthesis.

265 In contrast, for the piperidine, t(1/2) was determined to be approximately 4

266 group from a diverse set of C-2-substituted piperidines that were synthesized through directed Ru-ca

267 For N-Boc-2-phenylpyrrolidine and -piperidine, the barriers to rotation of the Boc group we

268 s are readily derivatized to enantioenriched piperidines, the most common N-heterocycle found in FDA

269 e report a catalytic asymmetric synthesis of piperidines through [4 + 2] cycloaddition of 1-azadienes

270 Compound 4 also reacts with piperidine to yield O-ethyl piperidinophosphate monoeste

271 mediated epimerization of readily accessible piperidines to provide the more stable diastereomer with

272 ing cyclic amines (pyrrolidine (TPMA(PYR) ), piperidine (TPMA(PIP) ), and morpholine (TPMA(MOR) )) by

273 namic resolution (CDR) of rac-2-lithio-N-Boc-piperidine using chiral ligand 8 or its diastereomer 9 i

274 ntheses of both enantiomers of 2-substituted piperidines using a wide range of electrophiles.

275 synthesis of optically active 3-substituted piperidines via ring expansion reaction.

276 oselective approach to cis-2,3-disubstituted piperidines via the reduction of N-acyliminium ion inter

277 heterologous competitive hapten containing a piperidine was further characterized.

278 ay of six pyridyl-substituted fused bicyclic piperidines was prepared as novel cores for medicinal ch

279 pical conformation of the penta(piperidinone-piperidine) was made.

280 ia iterative couplings; a penta(piperidinone-piperidine) was prepared in this way.

281 ammonium bicarbonate, ammonium formate, and piperidine) was studied.

282 -Sta-Leu-NH(2) (Pip, 4-amino-1-carboxymethyl-piperidine), was conjugated to 1,4,7-triazacyclononane,

283 R-specific (18)F-fluoroalkylated spirocyclic piperidines, we have chosen (18)F-fluspidine for detaile

284 d deprotection, enantiopure polyhydroxylated piperidines were isolated as single diastereoisomers (>9

285 Twenty-two aryl/heteroaryl pyrrolidines and piperidines were prepared using this method.

286 ylamino)-6-phenylpyrimidin-4-one-substituted piperidines were shown to inhibit GCC-mediated cellular

287 then be used to convert these molecules into piperidines, which are important structural components o

288 ituted aldehydes yield cis-2,5-disubstituted piperidines, while 3-substituted aldehydes afford trans-

289 the element effect order in the reaction of piperidine with 2,4-dinitrophenyl halides in methanol is

290 Reactions of piperidine with para-substituted styrenes are indicative

291 onstants for the reactions of morpholine and piperidine with the (2-methylindol-3-yl)phenylmethylium

292 enes when treated with triphenylphosphine or piperidine with the catalyst ReIO(2)(PPh(3))(2) (I).

293 r a large variety of di- to tetrasubstituted piperidines with aryl, alkyl, and carboxylic acid deriva

294 ermolecular cyclocondensation of substituted piperidines with arylaldehydes provides diversified 3,5-

295 rgo rearrangement to yield 2,3-disubstituted piperidines with excellent diastereoselectivity and enan

296 pyridinium salts provided 2-aryl-substituted piperidines with high levels of enantioselectivity.

297 Piperidines with substituents at the 2-position did not

298 zin-1-yl)-N-et hylnicotinamide] (piperazinyl-piperidine) with a rigid elongated structure containing

299 Compound 1 (4-(2-benzylphenoxy)piperidine) with high ligand efficiency for the histamin

300 Piperidines without substitution on nitrogen as well as