3-Hydroxy-5-(trifluoromethyl)thiophene-2-carboxylic acid → N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]-3-hydroxy-5-(trifluoromethyl)thiophene-2-carboxamide

HRID 13211노트

반응식

HRID 13211 반응식
[F:1][C:2]1[CH:7]=[CH:6][C:5]([N:8]2[C:16]3[C:11](=[CH:12][C:13]([O:17][C@H:18]([C:22]4[CH:27]=[CH:26][CH:25]=[C:24]([O:28][CH3:29])[CH:23]=4)[C@@H:19]([NH2:21])[CH3:20])=[CH:14][CH:15]=3)[CH:10]=[N:9]2)=[CH:4][CH:3]=1.[OH:30][C:31]1[CH:35]=[C:34]([C:36]([F:39])([F:38])[F:37])[S:33][C:32]=1[C:40](O)=[O:41]>>[F:1][C:2]1[CH:3]=[CH:4][C:5]([N:8]2[C:16]3[C:11](=[CH:12][C:13]([O:17][C@H:18]([C:22]4[CH:27]=[CH:26][CH:25]=[C:24]([O:28][CH3:29])[CH:23]=4)[C@@H:19]([NH:21][C:40]([C:32]4[S:33][C:34]([C:36]([F:39])([F:37])[F:38])=[CH:35][C:31]=4[OH:30])=[O:41])[CH3:20])=[CH:14][CH:15]=3)[CH:10]=[N:9]2)=[CH:6][CH:7]=1

참가 물질

3

반응물 2

HCID 27593483-Hydroxy-5-(trifluoromethyl)thiophene-2-carboxylic acidHCID 59339733(1R,2S)-1-(1-(4-fluorophenyl)indazol-5-yloxy)-1-(3-methoxyphenyl)propan-2-amine

생성물 1

HCID 59339799N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-(3-methoxyphenyl)propan-2-yl]-3-hydroxy-5-(trifluoromethyl)thiophene-2-carboxamide

실험 절차

Prepared as described in Example 269 from (1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)-1-(3-methoxyphenyl)propan-2-amine (6a, 50 mg, 0.13 mmol) and 3-hydroxy-5-(trifluoromethyl)thiophene-2-carboxylic acid (32 mg, 0.15 mmol).

후처리

  1. customPrepared

출처 및 근거

ORD 기록
ord-72c3b083e7d24c9593077d8e8bee133e
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07728030B2

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