Trifluoroacetic acid → 4-[3-(4-Hydroxymethyl-thiazol-2-yl)-phenyl]-7-(methyl-propyl-amino)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

HRID 1265931노트

반응식

HRID 1265931 반응식
C(OC(=O)[NH:7][C:8]1[CH:13]=[C:12]([N:14]([CH3:18])[CH2:15][CH2:16][CH3:17])[C:11]([C:19]([F:22])([F:21])[F:20])=[CH:10][C:9]=1[NH2:23])(C)(C)C.C(O[C:30](=[O:53])[CH2:31][C:32](=O)[C:33]1[CH:38]=[CH:37][CH:36]=[C:35]([C:39]2[S:40][CH:41]=[C:42]([CH2:44][O:45]C3CCCCO3)[N:43]=2)[CH:34]=1)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[OH:45][CH2:44][C:42]1[N:43]=[C:39]([C:35]2[CH:34]=[C:33]([C:32]3[CH2:31][C:30](=[O:53])[NH:23][C:9]4[CH:10]=[C:11]([C:19]([F:20])([F:21])[F:22])[C:12]([N:14]([CH3:18])[CH2:15][CH2:16][CH3:17])=[CH:13][C:8]=4[N:7]=3)[CH:38]=[CH:37][CH:36]=2)[S:40][CH:41]=1

참가 물질

5

반응물 3

HCID 6422Trifluoroacetic acidHCID 69486655Carbamic acid,[2-amino-5-(methylpropylamino)-4-(trifluoromethyl)phenyl]-,1,1-dimethylethyl esterHCID 696884923-Oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-thiazol-2-yl]-phenyl]-propionic acid tert-butyl ester

생성물 1

HCID 102065404-[3-(4-Hydroxymethyl-thiazol-2-yl)-phenyl]-7-(methyl-propyl-amino)-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

The title compound was prepared from [2-amino-5-(methyl-propyl-amino)-4-trifluoromethyl-phenyl]-carbamic acid tert-butyl ester (0.17 g) (Example J35) and 3-oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-thiazol-2-yl]-phenyl]-propionic acid tert-butyl ester (Example K27) (0.23 g) according to the general procedure M. The obtained material was deprotected and cyclized by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a yellow solid (0.06 g).

출처 및 근거

ORD 기록
ord-3eab7b3a6af94751a422fcbef1006b0d
출처 데이터셋
uspto-grants-2003_04
특허 번호
US06544985B2

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