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

HRID 1265912ノート

反応式

HRID 1265912 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:50])[CH2:28][C:29](=O)[C:30]1[CH:35]=[CH:34][CH:33]=[C:32]([C:36]2[S:37][CH:38]=[C:39]([CH2:41][O:42]C3CCCCO3)[N: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[S:37][CH:38]=[C:39]([CH2:41][OH:42])[N:40]=4)[CH:31]=3)[CH2:28][C:27](=[O:50])[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 696884923-Oxo-3-[3-[4-(tetrahydro-pyran-2-yloxymethyl)-thiazol-2-yl]-phenyl]-propionic acid tert-butyl ester

生成物 1

HCID 101390868-Chloro-4-[3-(4-hydroxymethyl-thiazol-2-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-[4-(tetrahydro-pyran-2-yloxymethyl)-thiazol-2-yl]-phenyl]-propionic acid tert-butyl ester (0.23 g) (Example K27) 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).

出典と根拠

ORDレコード
ord-50f408b6943c49c39215c53ecf4abbf6
出典データセット
uspto-grants-2003_04
特許番号
US06544985B2

反応ノート

読み込み中…