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

HRID 1265873ノート

反応式

HRID 1265873 の反応式
O[CH2:2][C:3]1[N:7]([C:8]2[CH:9]=[C:10]([C:14]3[CH2:20][C:19](=[O:21])[NH:18][C:17]4[CH:22]=[C:23]([CH3:32])[C:24]([N:26]([CH2:28][CH:29]([CH3:31])[CH3:30])[CH3:27])=[CH:25][C:16]=4[N:15]=3)[CH:11]=[CH:12][CH:13]=2)[N:6]=[N:5][CH:4]=1.S(Cl)(Cl)=O.[Cl-].[CH:38]1([CH2:41][NH2:42])[CH2:40][CH2:39]1>ClCCl.CN(C=O)C>[CH:38]1([CH2:41][NH:42][CH2:2][C:3]2[N:7]([C:8]3[CH:9]=[C:10]([C:14]4[CH2:20][C:19](=[O:21])[NH:18][C:17]5[CH:22]=[C:23]([CH3:32])[C:24]([N:26]([CH2:28][CH:29]([CH3:31])[CH3:30])[CH3:27])=[CH:25][C:16]=5[N:15]=4)[CH:11]=[CH:12][CH:13]=3)[N:6]=[N:5][CH:4]=2)[CH2:40][CH2:39]1

参加物

7

反応物 4

HCID 312ChlorideHCID 24386Thionyl ChlorideHCID 75646CyclopropanemethanamineHCID 186131914-[3-(5-Hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-7-(isobutyl-methyl-amino)-8-methyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

生成物 1

HCID 101631704-(3-{5-[(Cyclopropylmethyl-amino)-methyl]-[1,2,3]triazol-1-yl}-phenyl)-7-(isobutyl-methyl-amino)-8-methyl-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 4-[3-(5-hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-7-(isobutyl-methyl-amino)-8-methyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one (Example 132) (250 mg, 0.58 mmol) by reaction with thionylchloride in dichloromethane and subsequent treatment of the corresponding chloride with cyclopropylmethylamine in DMF according to the method described in Example 45. Obtained as a light yellow solid (50 mg, 18%).

出典と根拠

ORDレコード
ord-55731a642c53477897ddb6d42bc0ffe7
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…