Trifluoroacetic acid → 8-Chloro-7-(ethyl-methyl-amino)-4-[3-(4-hydroxymethyl-oxazol-2-yl)-phenyl]-1,3-dihydro-benzo[b][1,4]diazepin-2-one

HRID 1265915노트

반응식

HRID 1265915 반응식
C(OC(=O)[NH:7][C:8]1[CH:13]=[C:12]([N:14]([CH2:16][CH3:17])[CH3:15])[C:11]([Cl:18])=[CH:10][C:9]=1[NH2:19])(C)(C)C.C(O[C:26](=[O:49])[CH2:27][C:28](=O)[C:29]1[CH:34]=[CH:33][CH:32]=[C:31]([C:35]2[O:36][CH:37]=[C:38]([CH2:40][O:41]C3CCCCO3)[N:39]=2)[CH:30]=1)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[Cl:18][C:11]1[C:12]([N:14]([CH2:16][CH3:17])[CH3:15])=[CH:13][C:8]2[N:7]=[C:28]([C:29]3[CH:34]=[CH:33][CH:32]=[C:31]([C:35]4[O:36][CH:37]=[C:38]([CH2:40][OH:41])[N:39]=4)[CH:30]=3)[CH2:27][C:26](=[O:49])[NH:19][C:9]=2[CH:10]=1

참가 물질

5

반응물 3

HCID 6422Trifluoroacetic acidHCID 696880223-Oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-oxazol-2-yl]-phenyl]-propionic acid tert-butyl esterHCID 69688249Carbamic acid,[2-amino-4-chloro-5-(ethylmethylamino)phenyl]-,1,1-dimethylethyl ester

생성물 1

HCID 101594198-Chloro-7-(ethyl-methyl-amino)-4-[3-(4-hydroxymethyl-oxazol-2-yl)-phenyl]-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-4-chloro-5-(ethyl-methyl-amino)-phenyl]-carbamic acid tert-butyl ester (0.15 g) (Example J7) and 3-oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-oxazol-2-yl]-phenyl]-propionic acid tert-butyl ester (0.22 g) (Example K11) 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 (0.10 g).

출처 및 근거

ORD 기록
ord-32c1252f130d47f0874361cc1e3acbef
출처 데이터셋
uspto-grants-2003_04
특허 번호
US06544985B2

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