ライフサイエンスコーパス: morpholine

1 brary of primary and secondary amines (e.g., morpholine)].

2 ound for compounds containing a weakly basic morpholine.

3 N-dimethylamine, N-methylamine, ammonia, and morpholine.

4 etrahydrofurans, phthalans, isochromans, and morpholines.

5 uding challenging tri- and tetra-substituted morpholines.

6 cise constructions of conformationally rigid morpholines.

7 for the conversion of 1,2-amino alcohols to morpholines.

8 n pyrazolopyrimidine inhibitors with bridged morpholines.

9 pocket in mTOR that can accommodate bridged morpholines.

10 ncy was observed when the saturated rings on morpholine 1 and N-acetyl piperazine 2 were changed by a

11 S,S)-(11)C-2-(alpha-(2-methoxyphenoxy)benzyl)morpholine ((11)C-MeNER) is a highly selective inhibitor

12 4-[4-(1-isopropyl-piperidin-4-yloxy)-benzyl]-morpholine (13g), was found to be a potent, highly selec

13 )phenyl-4-(3-ox o-1 ,2,4-triazol-5-yl)methyl morpholine (17).

14 rimary amines (1 degrees ), piperidines, and morpholines (2 degrees ) were hydroxylated at the gamma-

15 o synthesize heterocycles, such as 2-hydroxy morpholine, 2-methyl quinoxalines, and benzodioxepinone

16 ated monomeric moieties (a modified lactide, morpholine-2,5-dione, and caprolactone), which under a t

17 -BOC-2-hydroxymethylmorpholine (1) and N-BOC-morpholine-2-carboxylic acid (2) from epichlorohydrin ha

18 3-trans- and 2,3-cis-6-methoxy-3-substituted morpholine-2-carboxylic esters were realized in few step

19 (4-(5-(6-fluoro-1H-indol-2-yl)pyrimidin-2-yl)morpholine; 21).

20 do-2-[(5-quinoxalinylsulfonyl)amino]benzoyl]-morpholine, 26d, a compound that demonstrates promising

21 For morpholines 27 and 29, the combination of steric and ele

22 Me), an amine (propargylamine, diethylamine, morpholine, 3,5-dimethylaniline, and isopropylamine), di

23 ide-like RGD-cyclopentapeptide, containing d-morpholine-3-carboxylic acid, interacts in vivo with alp

24 than those containing OAc (3a), NMe(2) (3e), morpholine (3f), OCH(2)CH CH(2) (3c), SPh (3g), or SePh

25 than those containing OAc (3a), NMe(2) (3e), morpholine (3f), OCH(2)CH=CH(2) (3c), SPh (3g), or SePh

26 e selective synthesis of trifluoromethylated morpholines (4-oxa-1-azabicyclo[4.1.0]heptanes) and so f

27 3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)morpholine-4-c arboxamido)pentanoate (6u) in a pig ische

28 sized a small-molecule inhibitor of MCD, 5-{(Morpholine-4-carbonyl)-[4-(2,2,2-trifluoro-1-hydroxy-1-t

29 1-(Morpholine-4-sulfonyl)-1H-benzotriazole 3c reacts with p

30 2), with pyrimidine (#5), pyrazole (#6), and morpholine (#9) being the big top 10 climbers.

31 To attenuate the basicity of morpholine, a bicyclic amine was designed and synthesize

32 g the ether-linked amines with carbon-linked morpholines, a modification motivated by free energy per

33 intermediacy of a 2-chloromethyl-substituted morpholine, accessed from epichlorohydrin and readily av

34 amethasone: 400 mg of an oral trisubstituted morpholine acetal (also known as L-754,030) before cispl

35 g novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor an

36 diastereomers, which were readily coupled to morpholine-activated dGMP.

37 cetate (2 mol %) in THF at room temperature, morpholine added to 5 in 81% yield.

38 m borohydride, methanesulfonyl chloride, and morpholine afforded the morpholinomethyl derivative 30.

39 A total synthesis of the purported morpholine alkaloid presented herein reveals discrepanci

40 e gave 2',6'-dimethyl-3'-pyridyl R-sec-butyl morpholine amide Epelsiban (69), a highly potent oxytoci

41 thermore, the ability to cleanly convert the morpholine amide to a methyl ketone was demonstrated.

42 A stable morpholine amide variant of thailandamide A has been acc

43 The morpholine amide variant of thailandamide A, synthesized

44 Both ketone- and morpholine amide-derived dienol ethers afforded high ena

45 he use of excess alkynyllithium reagent with morpholine amides provides a synthetically useful synthe

46 direct comparison between Weinreb amides and morpholine amides was made with regard to their reaction

47 reover, the reaction has been developed with morpholine amides, the products of which are precursors

48 eactions are obtained from the corresponding morpholine amides.

49 tion of pre-metalated reagents to Weinreb or morpholine amides.

50 An unanticipated change in reactivity in morpholine analogues is explained through interactions w

51 re somewhat larger as compared to the parent morpholine and bicyclic 3-oxa-7-azabicyclo[3.3.0]octane.

52 23-89% yield using optically active 2-benzyl morpholine and N-methyl camphanyl piperazine.

53 vitro and in vivo activity reveals that the morpholine and N-methylpiperazine Mannich side chains pr

54 The morpholine and phosphate rate constants at pH 8.9 are si

55 etera[3.3.n]propellanes (n = 2-4 ), advanced morpholine and piperazine analogues, is developed.

56 ublished rate constants for the reactions of morpholine and piperidine with the (2-methylindol-3-yl)p

57 practical strategies toward the synthesis of morpholines and Claisen rearrangement products based on

58 exes provides access to alpha-functionalized morpholines and piperazines directly from their parent a

59 clic trifluoromethylketones yields alpha-CF3 morpholines and piperazines.

60 thodology was further extended to synthesize morpholines and their homologues with high enantiospecif

61 red thiazolidine, six-membered 1,4-oxazines (morpholines) and tetrahydro-2H-1,4-thiazines (thiomorpho

62 of the anticancer drug Sonidegib (instead of morpholine), and Danofloxacine (instead of piperazine) p

63 ary and secondary amines such as butylamine, morpholine, and aniline derivatives.

64 roacetamides, on heating with benzotriazole, morpholine, and triethylamine, produce, in a one-pot rea

65 nes and diamines (pyrrolidines, piperidines, morpholines, and piperazines) by the cumyloxyl (CumO(*))

66 cal animal models sets it apart from earlier morpholine antagonists (such as 4), and the piperidine a

67 from nonvolatile diethanolamine to volatile morpholine, application of 272-537 mJ/cm(2) UV incident

68 Morpholines are common heterocycles in pharmaceutical an

69 Morpholines are prevalent in medicinal chemistry due to

70 4-(Pyrimidin-4-yl)morpholines are privileged pharmacophores for PI3K and P

71 h an optimized stabilizing alkyl-substituted morpholine as 3'-overhangs resulted in siRNAs without an

72 ines in a lab-scale CO2 capture reactor with morpholine as a model solvent amine.

73 The experiments were conducted using morpholine as a representative secondary amine as a pote

74 ategy also provides access to fused bicyclic morpholines as well as 2,3- and 2,5-disubstituted produc

75 pH range from 10.12 to 11.66 and those with morpholine at pH 12.0 are characterized by two kinetic p

76 In contrast, for the reaction of 4-SMe with morpholine at pH 8.62 the rates of product formation and

77 A morpholine-based nucleotide analog was developed as a bu

78 sults suggest that the use of (125)I-labeled morpholine-based RGD-cyclopentapeptides targeting alpha(

79 tion, and from N-(6-chloropyridin-3-ylmethyl)morpholine by an electrophilic azide introduction with l

80 alpha-Functionalized morpholines can be elaborated further, for instance by i

81 on mechanism of the dipeptidyl boronate N-(4-morpholine)carbonyl-beta-(1-naphthyl)-L-alanine-L-leucin

82 convergent syntheses of 2- and 3-substituted morpholine congeners are reported.

83 The morpholine-conjugated fluorescent probe usually localize

84 an be used for the synthesis of a variety of morpholines containing substituents at various positions

85 Downregulation of Unx1 mRNA with morpholine contains Trypanosoma cruzi invasion.

86 Petasis condensation with glyoxylic acid and morpholine controlled by the helical chirality afforded

87 triazolinone side chain was appended to the morpholine core.

88 hibitor Z-Leu-aminobutyric acid-CONH(CH(2))3-morpholine (CX295).

89 large spectral shift (2.0 nm/deg twist) for morpholine deformations within these fairly flexible moi

90 nt representatives of this class include the morpholine derivative linezolid 2, which is currently in

91 identified amorolfine (AMF), a phenyl-propyl morpholine derivative, as a putative modulator.

92 t process to the desired alpha-(fluorophenyl)morpholine derivative.

93 Our method expands access to morpholine derivatives bearing multiple substituents alp

94 ents alpha to oxygen and densely substituted morpholine derivatives bearing up to six C substituents.

95 ed in medicinal chemistry, but C-substituted morpholine derivatives remain challenging to access.

96 a new approach to C-substituted unsaturated morpholine derivatives that are poised to undergo furthe

97 synthesize highly substituted, N-unprotected morpholine derivatives via aziridinyl alcohols.

98 e and combinatorial synthesis of substituted morpholine derivatives with handles for further elaborat

99 acetal of the above lactone, whereas 2,3-cis-morpholines derive from the R*,R*-product of basic conde

100 In particular, 2,3-trans-morpholines derive from the R*,S*-product of the acid co

101 The enantioselectivities achieved with the morpholine derived-dienolate in the addition to aliphati

102 vity over a broad scope; a case study with a morpholine-derived substrate illustrates the negative im

103 d and Drug Administration's requirements for morpholine detection in real-life applications.

104 Co-injection of sub-inhibitory levels of morpholines directed against both Tsg and chordin synerg

105 ive annulation strategy for the synthesis of morpholines directly from readily available starting mat

106 crystal structure of the hCA II adduct with morpholine dithiocarbamate evidenced the inhibition mech

107 nthesized via hydroboration/oxidation of the morpholine enamine of (+)-nopinone.

108 amine protocol (SnAP) reagents and a single morpholine-forming assembly reaction.

109 also demonstrated the formal synthesis of a morpholine from a simple primary amine using ethylene su

110 e to the traditional methods used to prepare morpholines from 1,2-amino alcohols, the most striking f

111 four-step synthesis of cis-3,5-disubstituted morpholines from enantiomerically pure amino alcohols is

112 ized for the synthesis of a diverse range of morpholine-fused triazoles of chemotherapeutic value.

113 Chiral morpholines gave inhibitors whose enantiomers had differ

114 at the reduction of CO(2) in the presence of morpholine (generating mixtures of the corresponding car

115 OTA-SFCVM, [(68)Ga]NOTA-SFCVHEM containing a morpholine group and a histidine-glutamate-histidine-glu

116 Replacement of the morpholine group of 2c with a 4-methylpiperazine group p

117 erazine groups can be replaced by less basic morpholine groups with no loss of intermolecular interac

118 Less basic analogues, such as morpholines, had good oral absorption; however, they als

119 lates 2, base catalysis is utilized to yield morpholine hemiaminals.

120 distinct chemotype that lacks the canonical morpholine hinge-binder of classical lipid kinase inhibi

121 eting selectivity were achieved by replacing morpholine in pyrazolopyrimidine inhibitors with bridged

122 iperazine, 1-(2-hydroxyethyl)piperazine, and morpholine in the same solvent.

123 6)-p-cymene), to afford chiral 3-substituted morpholines in good yield and enantiomeric excesses of >

124 d by palladium chloride leads to substituted morpholines in good yields.

125 ons beyond those related to the synthesis of morpholines, including obtaining proof-of-principle that

126 thyl acrylamide)), and PAcM (poly(N-acryloyl morpholine)), increases circulation times of liposomes;

127 Six morpholine-(iso)thiosemicarbazone hybrids HL(1)-HL(6) an

128 iscovery of a potent non-nitrogen containing morpholine isostere with the ability to mimic this confo

129 iperazine, 1-(2-hydroxyethyl)piperazine, and morpholine it is deprotonation of T(+/-)(A) that is rate

130 dt-Kindler reaction to the N-piperidine or N-morpholine julolidine-9-thioamide.

131 )phenyl-4-((3-oxo-1,2,4-tri azol-5-yl)methyl)morpholine (L-742694) is a potent activator of the rat P

132 to be highly reactive for the formylation of morpholine, leading to the formation of N-formylmorpholi

133 The morpholine ligand also plays a pivotal role in tuning op

134 nt probe, PM-Mor-OH, based on the lipophilic morpholine ligand-conjugated pyridinium derivative of "I

135 The morpholine-like fungicides, fenpropimorph and spiroxamin

136 ear-planar meso-tetraarylbacteriochlorins to morpholine moieties yields ruffled mono- and bismorpholi

137 alpha-Calpha-Cbeta dihedral angle within the morpholine moieties.

138 odified chlorins incorporating oxazolone and morpholine moieties.

139 Evidently, the position of the morpholine moiety and the copper(II) complex formation h

140 This morpholine moiety deformation can take place largely ind

141 Intramolecular ring-closure reactions of the morpholine moiety with the flanking meso-aryl groups lea

142 ed for the spectrofluorimetric assessment of morpholine (MOR) where BF exhibits morpholine-sensing be

143 ; L1 = N-(2-(di(1-adamantyl)phosphino)phenyl)morpholine, Mor-DalPhos).

144 stants is as follows: diethanolamine (DEA) < morpholine (MORP) ~ thiomorpholine (TMORP) < N-methylpip

145 The morpholine motif is valued in medicinal chemistry, but C

146 V)-carbene [(BIPM)UCl(3)Li(THF)(2)] (4) by 4-morpholine N-oxide afforded the first uranium(VI)-carben

147 eb amide), N-ethyl-N-phenylbenzamide, N-acyl morpholine, N-acyl valerolactam, and N-acyl caprolactam.

148 ction of a hydrogen-bonding acceptor such as morpholine nearby the phenolic hydroxyl group, which als

149 In light of the basicity of the morpholine nitrogen in the AAIs, separate CoMFA models w

150 Further, simple alkylation of the morpholine nitrogen led to a nucleotide analog, which in

151 ith an adjacent aromatic core favored by the morpholine nitrogen nonbonding pair of electrons interac

152 aloglycoprotein-binding GalNAc ligand at the morpholine nitrogen was realized with different linkers.

153 nine in all types of DNA were lower than the morpholine nitrosation rate constant by a factor of appr

154 n of stereoelectronic effects, and, with the morpholines, on the basis of polar effects.

155 or AK295 [Z-Leu-aminobutyric acid-CONH(CH2)3-morpholine] on cognitive and motor deficits following la

156 one of those pharmacophores in place at C24, morpholines or carbamates were installed at the C3 posit

157 henone or phenylacetaldehyde and piperidine, morpholine, or pyrrolidine were located using quantum me

158 A range of enantioenriched spiro[3,2'-morpholine-oxindole] derivatives which incorporate a ter

159 r PI3K and PIKKs inhibition by virtue of the morpholine oxygen, both forming the key hydrogen bonding

160 se inhibitors is a critical hydrogen bond to morpholine oxygen, initially present in the early nonspe

161 ligand N-(4-(di(1-adamantyl)phosphino)phenyl)morpholine (p-Mor-DalPhos, L2) was prepared in 63% yield

162 Rate constants for reaction of morpholine, phosphate, and bicarbonate with N2O3 relativ

163 methylthio-alpha-nitrocinnamate (4-SMe) with morpholine, piperidine, and hydroxide ion in 50% DMSO/50

164 e or no oligomer formation was observed when morpholine, piperidine, pyrazole, 1,2,4-triazole, and 2-

165 that among all of the studied compounds, the morpholine/piperidine-substituted pyrido[1,2-e]purine de

166 thienyl, ferrocenyl), ArC=C, amine (NHPh and morpholine), PO(OEt)(2), sulfanyl (SBu- t), alkoxide (OE

167 The morpholine products are generated as single stereoisomer

168 We report the synthesis of two novel bridged morpholine-proline chimeras 4 and 5, which represent rig

169 ith good hydrogen bonding potential, such as morpholine, pyridine, and imidazole, shift the melting t

170 designed bidentate oxime ether-pyridone and morpholine-pyridone ligands are crucial for this tandem

171 Few selective morpholine replacements have been identified to date.

172 zation to form pyrrolidines, piperidines, or morpholines results in a preorganization of the whole sy

173 An extensive investigation of the morpholine ring engaging the mTOR solvent exposed region

174 exocyclic enol ether, from which the second morpholine ring is constructed in two steps.

175 ome P450 3A4 inhibition, possibly related to morpholine ring metabolism.

176 azole moieties have been used to replace the morpholine ring of linezolid (2).

177 ationally constrained analogues in which the morpholine ring of linezolid is replaced with various su

178 ng an unusual cis-2,6-disubstituted bis-aryl morpholine ring to which is attached a (Z)-4-hydroxycinn

179 plex molecules through the carbon atoms of a morpholine ring, affording rapid access to diverse molec

180 s an antagonist with IC(50) of 805 nM, while morpholine ring-containing analogues were nearly inactiv

181 It is found that H(2)O(2) oxidizes both morpholine ring-containing buffers (e.g., Mops, Mes) and

182 version of the adjacent chiral center on the morpholine ring.

183 ibited in cultured embryonic pancreata using morpholine-ring antisense against GIP ligand and recepto

184 Morpholine-ring antisense or siRNA against either GIP li

185 efined sp(3)-rich scaffold incorporating two morpholine rings embedded within a spiroacetal framework

186 ws ready substitution of one-or both- of the morpholine rings for 1,4-oxazepanes and the generation o

187 1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862), which showed high activity i

188 ssment of morpholine (MOR) where BF exhibits morpholine-sensing behavior.

189 g a polar group such as diethylene glycol or morpholine significantly improved their physical propert

190 CO(2) is apt to be captured by morpholine solution, while a highly efficient heterogene

191 Analysis of aqueous morpholine solutions purged with different gas-phase NO

192 icyclo[2.2.1]heptanes as carbon-atom bridged morpholines, starting with 4R-hydroxy-l-proline as a chi

193 -amino-substituted benzo[h]chromen-4-ones, a morpholine substituent at this position was essential fo

194 Exchange of a morpholine substituent for an (S)-3-hydroxypyrrolidine r

195 ion had been "knocked-out" by injection of a morpholine-substituted antisense oligonucleotide to gene

196 Loss-of-function assays with morpholine-substituted antisense oligonucleotides show t

197 Existing methods for morpholine synthesis often require prefunctionalized or

198 tes how the unique molecular features of the morpholine synthon bestows selectivity against class I P

199 bitor, which contains a 2,6,6-trisubstituted morpholine system, can be accomplished.

200 er, herein, we observed unusual phenomena of morpholine-tagged PM-Mor-OH that localized mitochondria

201 calization when appended with the well-known morpholine targeting motif.

202 pounds bearing different heterocycles (e.g., morpholine, tetrahydroisoquinoline, benzimidazole, piper

203 cation of heterocycles including piperidine, morpholine, thiane, tetrahydropyran, and tetrahydroisoqu

204 Beyond morpholines, this strategy is extended to piperidines, p

205 enantioselective synthesis of 3-substituted morpholines through a tandem sequential one-pot reaction

206 Besides, sequential addition of morpholine to the in situ-generated unstable chlorine ca

207 e (TPMA(PYR) ), piperidine (TPMA(PIP) ), and morpholine (TPMA(MOR) )) by nucleophilic aromatic substi

208 In addition, the CO(2) captured by morpholine under atmospheric conditions can be converted

209 Additionally, the morpholines, unlike the pyrrolidine and piperidine analo

210 After incubation with 1-200 nm morpholine urea-leucine-homophenylalanine-phenyl vinyl s

211 n rate constants were determined relative to morpholine using a Silastic membrane to deliver NO. at a

212 h by investigating excited state dynamics in morpholine using time-resolved photoelectron imaging.

213 Key to the morpholine utility as a kinase hinge binder is its abili

214 -oxadiazol-5-yl}methyl)piperidin-3-yl]methyl}morpholine, V-0219) that exhibits enhanced efficacy of G

215 zino[4',5':4,5]thieno[2,3-c]isoquinolin-5-yl)morpholine was administered to mice to selectively inhib

216 When morpholine was present in the reaction system, N-nitroso

217 sed isosteres of piperidine, piperazine, and morpholine were designed and synthesized on up to gram s

218 ts of different concentrations of nitrite on morpholine were evaluated.

219 ous dihetera[3.3.n]propellanes, analogues of morpholine, were obtained from X-ray diffraction studies

220 brary of primary and secondary amines, e.g., morpholine] were placed at the 1-position.

221 hibitory ligands (e.g. 4-phenylimidazole and morpholine) while discriminating against larger azole dr

222 d for the [Pd(NHC)(2)]-catalyzed coupling of morpholine with 4-chlorotoluene are consistent with a ra

223 ylamide followed by chlorine substitution of morpholine with ethyl chloroformate.

224 y the deprotonation of 4-(N-tetrazolylmethyl)morpholine with LiHMDS, undergoes addition to ketones an

225 ns are made with reactions of piperidine and morpholine with other highly activated vinylic substrate

226 The activation energy for the reaction of morpholine with sodium nitrite was found as 101 kJ/mol.

227 2-methyl-6-methyleneoctan-2-ol, 4-octadecyl-morpholine, (Z)-methyl-3-hexenoate and 3-octanone) are r