ライフサイエンスコーパス: piperidine

1 ctical procedure for the synthesis of chiral piperidines.

2 d for the synthesis of functionalized chiral piperidines.

3 ient entry to this class of pyrrolidines and piperidines.

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

5 d diazoketones for the rapid construction of piperidines.

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

7 tial activities of the above piperazines and piperidines.

8 drobase intermediates afforded 4-substituted piperidines.

9 cluding pyridines, pyrimidines, indoles, and piperidines.

10 yl aziridines, azetidines, pyrrolidines, and piperidines.

11 versatile synthesis of structurally complex piperidines.

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

13 omega-unsaturated N-sulfanilamide to furnish piperidines.

14 uilding block for the synthesis of annulated piperidines.

15 zones to afford substituted pyrrolidines and piperidines.

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

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

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

19 n inhibitor, N-phenyl-4-(quinolin-3-ylmethyl)piperidine-1-carboxamide (PF-750), that shows strong pre

20 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)piperidine-1-carboxylate (JZL184)] prolong DSE in autapt

21 ahydrofuran-2-yl)-9H-pur in-2-yl)prop-2-ynyl)piperidine-1-carboxylic acid methyl ester (ATL313) or 2-

22 2573X (4-(2-methoxyphenylcarbamoyloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester).

23 ), 4-oxo-TEMPO(*) (2,2,6,6-tetramethyl-4-oxo-piperidine-1-oxyl radical), di-tert-butylnitroxyl ((t)Bu

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

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

26 natural amino acid TOAC (2,2,6,6-tetramethyl-piperidine-1-oxyl-4-amino-4-carboxylic acid), which is c

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

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

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

30 3-ylm ethyl)-2-oxoethyl]spiro[1H-indene-1,4'-piperidine]-1'-carboxamide) in DA amacrine cells and the

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

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

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

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

38 onfigured substituents, respectively, at the piperidine 3'-position exhibited comparable cytotoxicity

39 -1-[3-(2,3,5-trifluoro-phenyl )-prop-2-ynyl]-piperidine-3-carboxylic acid (RPR260243), reverse the ef

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

41 ]-1-[3-(2,3,5-trifluorophenyl )-prop-2-ynyl]-piperidine-3-carboxylic acid] (RPR) slows deactivation a

42 -1-[3-(2,3,5-trifluoro-pheny l)-prop-2-ynyl]-piperidine-3-carboxylic acid] (RPR), a recently discover

43 l]-1-[3-(2,3,5 trifluorophenyl)-prop-2-ynyl]-piperidine-3-carboxylic acid], a type 1 agonist, binds t

44 y reactions of acylbenzotriazoles 2a-2p with piperidines 3a-3f.

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

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

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

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

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

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

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

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

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

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

55 (2,4-diaminopteridin-6-ylmethylamino)benzoyl]piperidine-4-carboxylate (1) led to the synthesis of a f

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

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

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

59 7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol and piperidine-4-sulfonic acid, we examined BDZ modulation u

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

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

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

63 These data suggest that spiro-piperidine 9 binds more extensively with the AM2 channel

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

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

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

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

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

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

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

71 formamidopyrimidine DNA glycosylase and hot piperidine, although GT-containing sequence contexts dis

72 t screening leads afforded a 1,4-substituted piperidine amide 6 with good potency and limited selecti

73 40, 41, 48, and 49, with C-28 piperazine or piperidine amide substitutions, increased the activity b

74 4-Aminoquinolone piperidine amides (AQs) were identified as a novel scaff

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

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

77 nity not achieved in similarly N-substituted piperidine analogues and significantly (470-fold) improv

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

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

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

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

82 Further SAR on reducing the basicity of the piperidine and introducing polarity led to the discovery

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

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

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

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

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

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

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

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

91 g a direct synthetic approach to substituted piperidines and piperidones.

92 to provide the corresponding functionalized piperidines and pyrrolidines.

93 O-H (2,2,6,6-tetramethyl-N-hydroxy-4-methoxy-piperidine), and (t)Bu(2)NOH.

94 lpha-nitrocinnamate (4-SMe) with morpholine, piperidine, and hydroxide ion in 50% DMSO/50% water (v/v

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

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

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

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

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

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

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

102 Piperidines are prevalent in natural products and pharma

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

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

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

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

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

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

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

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

113 Piperidine carboxamide 1 was identified as a novel inhib

114 -[4-chlorophenyl]-1-[3-(2-furanyl)benzoyl]-3-piperidine carboxamide) and/or Fas-activating antibody i

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

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

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

118 covery of 64 and 68 in the 4,4-disubstitited piperidine class H, both potent CCR5 ligands (pIC 50 = 8

119 om the trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of opioid antagonist.

120 om the trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of opioid antagonists.

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

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

123 The piperidine compound 11a up-regulated expression of the m

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

125 le to identify a series of piperidinone- and piperidine-constrained phenethylamines as novel DPP4 inh

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

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

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

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

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

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

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

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

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

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

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

137 ynthesis of polysubstituted cyclopentane and piperidine derivatives.

138 ng structurally and stereochemically diverse piperidine derivatives.

139 Piperidine-derived analogues showing minimal microsomal

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

141 4-Substituted piperidine-derived trisubstituted ureas are reported as

142 finity glutamate receptor antagonist cis-2,3-piperidine dicarboxylic acid (PDA) increased paired-puls

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

144 The origin of the piperidine effect primarily derives from the in situ gen

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

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

147 wed that the reactivity toward deblocking by piperidine followed the order alpha-Nsmoc > Bsmoc > beta

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

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

150 ccess to a variety of 2-arylpyrrolidines and piperidines from commercially available proline, hydroxy

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

152 Piperidine-functionalized, 1,4-disubstituted-1,2,3-triaz

153 2-(2-propynyl)pyrrolidine and 2-(2-propynyl)piperidine gave 2-(9-phenanthylmethyl)pyrrolidines and 2

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

155 wth as well as incorporation of solubilizing piperidine groups.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

174 one strand consistently involved a modified (piperidine-labile) guanine and was not reversed by heat,

175 Structural modification of the piperidine leads 1 and 2 afforded the fluorinated piperi

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

177 In double-stranded DNA, hot piperidine-mediated cleavage at G2 occurs only after G1P

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

182 ubstituted alkene through which the bicyclic piperidine moiety can readily be accessed.

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

184 ntermediates to construct the functionalized piperidine moiety in the key steps.

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

186 logues with various functional groups on the piperidine moiety were designed, synthesized, and evalua

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

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

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

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

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

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

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

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

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

196 beta-fluorination modulated the p K a of the piperidine nitrogen and reduced Pgp efflux, but the resu

197 2, protonation or Mg(2+) complexation of the piperidine nitrogen removes the intramolecular hydrogen

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

199 mmonium hydroxide (TBAH), and an amine base, piperidine, on the direct synthesis of pyridine-3,5-dica

200 cant selectivity under the 1-benzenesulfinyl piperidine or diphenyl sulfoxide conditions.

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

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

203 he thioglycosides with the 1-benzenesulfinyl piperidine, or diphenyl sulfoxide, and trifluoromethanes

204 sphine at room temperature by treatment with piperidine, or simply by refluxing in methanol.

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

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

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 he Sigma-1 ligand 4-phenyl-1-(4-phenylbutyl) piperidine (PPBP) protects the brain from ischemia.

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

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

215 e substituted pyridine, dihydropyridine, and piperidine products.

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

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

218 More rigid piperidines provided the highest selectivity of the reac

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 emistry (formamidopyrimidine DNA glycosylase/piperidine ratio).

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

229 clizations, furnishing either pyrrolidine or piperidine, respectively.

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

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

232 udies indicated that the sulfonyl group, the piperidine ring and benzothiazole were the key component

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

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 Ring size reduction of the central piperidine ring of lobelane yielded pyrrolidine analogue

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

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

240 33 different organocations derived from the piperidine ring system.

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

242 7 indicated that the benzylated six-membered piperidine ring was disordered and exposed to solvent.

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

244 reductive amination sequence that closes the piperidine ring.

245 nteractions to control the conformation of a piperidine ring.

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

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

248 f enantioenriched pyrrolidine, indoline, and piperidine rings using an organocatalyzed, intramolecula

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

250 oducts containing only fused pyrrolidine and piperidine rings.

251 idine leads 1 and 2 afforded the fluorinated piperidine ( S)- 5, a potent and selective antagonist th

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

253 ermined that a substoichiometric quantity of piperidine (secondary amine) in combination with cesium

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

255 xo-1,2-dihydrospirobenzo[d][1,3]oxazine-4,3'-piperidine series of spirocycles (e.g., 42) and their pr

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

257 by the concentration and temperature of the piperidine solution as well as the number of Fmoc moieti

258 pened" by the cleavage of Fmoc groups with a piperidine solution.

259 complementary strand scission occurred at a piperidine-stable -1 nt and was reversed by EDTA.

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

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

262 In our laboratories, piperidine-substituted quinazolinone derivatives were id

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

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

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

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

267 lizing a functionalized pyridine moiety as a piperidine surrogate.

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

269 limitations of the carbamate annulation for piperidine synthesis.

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

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

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

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

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

275 Significantly, piperidine treatment of the mitochondria leads to protei

276 ns, with activation by the 1-benzenesulfinyl piperidine/triflic anhydride system.

277 beta-glycosides using the 1-benzenesulfinyl piperidine/trifluoromethanesulfonic anhydride protocol.

278 hesis of an N-methyl-3-fluoro-4-(aminomethyl)piperidine urea led to compound 30 that has an optimal i

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

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

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

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

283 heterologous competitive hapten containing a piperidine was further characterized.

284 n, analogues have been synthesized where the piperidine was replaced by a tropane ring that reversed

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

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

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

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

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

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

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

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

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

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

295 Reactions of piperidine with para-substituted styrenes are indicative

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

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

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

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

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