Chloride → 8-Chloro-4-{3-[5-(isobutylamino-methyl)-[1,2,3]triazol-1-yl]-phenyl}-7-(isopropyl-methyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

HRID 1265885ノート

反応式

HRID 1265885 の反応式
[Cl:1][C:2]1[C:3]([N:27]([CH:29]([CH3:31])[CH3:30])[CH3:28])=[CH:4][C:5]2[N:11]=[C:10]([C:12]3[CH:17]=[CH:16][CH:15]=[C:14]([N:18]4[C:22]([CH2:23]O)=[CH:21][N:20]=[N:19]4)[CH:13]=3)[CH2:9][C:8](=[O:25])[NH:7][C:6]=2[CH:26]=1.S(Cl)(Cl)=O.[Cl-].[CH2:37]([NH2:41])[CH:38]([CH3:40])[CH3:39]>ClCCl.CN(C=O)C>[Cl:1][C:2]1[C:3]([N:27]([CH:29]([CH3:30])[CH3:31])[CH3:28])=[CH:4][C:5]2[N:11]=[C:10]([C:12]3[CH:17]=[CH:16][CH:15]=[C:14]([N:18]4[C:22]([CH2:23][NH:41][CH2:37][CH:38]([CH3:40])[CH3:39])=[CH:21][N:20]=[N:19]4)[CH:13]=3)[CH2:9][C:8](=[O:25])[NH:7][C:6]=2[CH:26]=1

参加物

7

反応物 4

HCID 312ChlorideHCID 6558IsobutylamineHCID 24386Thionyl ChlorideHCID 186131088-Chloro-4-[3-(5-hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-7-(isopropyl-methyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

生成物 1

HCID 186133708-Chloro-4-{3-[5-(isobutylamino-methyl)-[1,2,3]triazol-1-yl]-phenyl}-7-(isopropyl-methyl-amino)-1,3-dihydro-benzo[b][1,4]diazepin-2-one

試薬・触媒・溶媒 2

HCID 6228Dimethylformamide溶媒HCID 6344Dichloromethane溶媒

実験手順

The title compound was prepared from 8-chloro-4-[3-(5-hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-7-(isopropyl-methyl-amino)-1,3-dihydro-benzo[b][1,4]-diazepin-2-one (Example 96) (220 mg, 0.50 mmol) by reaction with thionylchloride in dichloromethane and subsequent treatment of the corresponding chloride with isobutylamine in DMF according to the method described in Example 45. Obtained as a light yellow solid (160 mg, 65%).

出典と根拠

ORDレコード
ord-eb5d993802874b0f8963a0c020a2b761
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…