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

HRID 1265928ノート

反応式

HRID 1265928 の反応式
C(OC(=O)[NH:7][C:8]1[CH:13]=[C:12]([N:14]([CH3:18])[CH2:15][CH2:16][CH3:17])[C:11]([Cl:19])=[CH:10][C:9]=1[NH2:20])(C)(C)C.C(O[C:27](=[O:43])[CH2:28][C:29](=O)[C:30]1[CH:35]=[CH:34][CH:33]=[C:32]([C:36]2[N:37]=[C:38]([CH3:41])[O:39][CH:40]=2)[CH:31]=1)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[Cl:19][C:11]1[C:12]([N:14]([CH3:18])[CH2:15][CH2:16][CH3:17])=[CH:13][C:8]2[N:7]=[C:29]([C:30]3[CH:35]=[CH:34][CH:33]=[C:32]([C:36]4[N:37]=[C:38]([CH3:41])[O:39][CH:40]=4)[CH:31]=3)[CH2:28][C:27](=[O:43])[NH:20][C:9]=2[CH:10]=1

参加物

5

反応物 3

HCID 6422Trifluoroacetic acidHCID 69688379Carbamic acid,[2-amino-4-chloro-5-(methylpropylamino)phenyl]-,1,1-dimethylethyl esterHCID 696892093-Oxo-3-[3-(2-methyl-oxazol-4-yl)-phenyl]-propionic acid tert-butyl ester

生成物 1

HCID 186134428-Chloro-4-[3-(2-methyl-oxazol-4-yl)-phenyl]-7-(methyl-propyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

The title compound was prepared from [2-amino-4-chloro-5-(methyl-propyl-amino)-phenyl]-carbamic acid tert-butyl ester (0.16 g) (Example J8) and 3-oxo-3-[3-(2-methyl-oxazol-4-yl)-phenyl]-propionic acid tert-butyl ester (0.17 g) (Example K29) 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 (0.07 g).

出典と根拠

ORDレコード
ord-bf5bbb09caa14875ae728843771287ad
出典データセット
uspto-grants-2003_04
特許番号
US06544985B2

反応ノート

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