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 n pyrazolopyrimidine inhibitors with bridged morpholines.

5 pocket in mTOR that can accommodate bridged morpholines.

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

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

8 4-[4-(1-isopropyl-piperidin-4-yloxy)-benzyl]-morpholine (13g), was found to be a potent, highly selec

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

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

11 3-trans- and 2,3-cis-6-methoxy-3-substituted morpholine-2-carboxylic esters were realized in few step

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

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

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

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

16 3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)morpholine-4-c arboxamido)pentanoate (6u) in a pig ische

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

18 1-(Morpholine-4-sulfonyl)-1H-benzotriazole 3c reacts with p

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

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

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

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

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

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

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

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

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

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

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

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

31 eactions are obtained from the corresponding morpholine amides.

32 23-89% yield using optically active 2-benzyl morpholine and N-methyl camphanyl piperazine.

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

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

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

36 clic trifluoromethylketones yields alpha-CF3 morpholines and piperazines.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

53 triazolinone side chain was appended to the morpholine core.

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

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

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

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

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

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

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

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

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

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

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

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

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

67 Chiral morpholines gave inhibitors whose enantiomers had differ

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

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

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

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

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

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

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

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

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

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

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

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

80 odified chlorins incorporating oxazolone and morpholine moieties.

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

82 This morpholine moiety deformation can take place largely ind

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

98 The morpholine products are generated as single stereoisomer

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

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

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

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

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

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

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

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

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

108 Morpholine-ring antisense or siRNA against either GIP li

109 1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862), which showed high activity i

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

129 2-methyl-6-methyleneoctan-2-ol, 4-octadecyl-morpholine, (Z)-methyl-3-hexenoate and 3-octanone) are r