(3S)-4-(tert-Butoxycarbonyl)morpholine-3-carboxylic acid → 3(S)-{4-[3-(5-Chloro-2-hydroxy-phenyl)-1-(2-hydroxy-ethyl)-1H-pyrazol-4-ylethynyl]-phenylcarbamoyl}-morpholine-4-carboxylic acid tert-butyl ester

HRID 2075765노트

반응식

HRID 2075765 반응식
[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][O:11][CH2:10][CH:9]1[C:14](=[O:40])[NH:15][C:16]1[CH:21]=[CH:20][C:19]([C:22]#[C:23][C:24]2[C:25]([C:32]3[CH:37]=[C:36]([Cl:38])[CH:35]=[CH:34][C:33]=3[OH:39])=[N:26][N:27]([CH2:29][CH2:30][OH:31])[CH:28]=2)=[CH:18][CH:17]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].NC1C=CC(C#CC2C(C3C=C(Cl)C=CC=3O)=NN(CCO)C=2)=CC=1.C(OC(N1CCOC[C@H]1C(O)=O)=O)(C)(C)C>>[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][O:11][CH2:10][C@H:9]1[C:14](=[O:40])[NH:15][C:16]1[CH:17]=[CH:18][C:19]([C:22]#[C:23][C:24]2[C:25]([C:32]3[CH:37]=[C:36]([Cl:38])[CH:35]=[CH:34][C:33]=3[OH:39])=[N:26][N:27]([CH2:29][CH2:30][OH:31])[CH:28]=2)=[CH:20][CH:21]=1)=[O:7])([CH3:4])([CH3:2])[CH3:3]

참가 물질

4

반응물 3

HCID 1512537(3S)-4-(tert-Butoxycarbonyl)morpholine-3-carboxylic acidHCID 1359749113(R,S)-{4-[3-(5-Chloro-2-hydroxy-phenyl)-1-(2-hydroxy-ethyl)-1H-pyrazol-4-ylethynyl]-phenylcarbamoyl}-morpholine-4-carboxylic acid tert-butyl esterHCID 1359749132-[4-(4-Amino-phenylethynyl)-1-(2-hydroxy-ethyl)-1H-pyrazol-3-yl]-4-chloro-phenol

생성물 1

HCID 1359750093(S)-{4-[3-(5-Chloro-2-hydroxy-phenyl)-1-(2-hydroxy-ethyl)-1H-pyrazol-4-ylethynyl]-phenylcarbamoyl}-morpholine-4-carboxylic acid tert-butyl ester

실험 절차

Using the same procedure for the preparation of 16A, reaction of compound 2A with (S)-morpholine-3,4-dicarboxylic acid 4-tert-butyl ester (19A) afforded the title compound 20A as a white powder in similar yield. Its 1H NMR and LCMS data are identical with those of compound 16A.

출처 및 근거

ORD 기록
ord-122a840df021442a90ffe4d14e885f40
출처 데이터셋
uspto-grants-2011_04
특허 번호
US07923004B2

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