Chloride → 7-(Isobutyl-methyl-amino)-8-methyl-4-[3-(5-pyrrolidin-1-ylmethyl-[1,2,4]triazol-1-yl)-phenyl]-1,3-dihydro-benzo[b][1,4]diazepin-2-one

HRID 1265887ノート

反応式

HRID 1265887 の反応式
OC[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-].N1[CH2:42][CH2:41][CH2:40][CH2:39]1.[CH3:43][N:44](C=O)C>ClCCl>[CH2:28]([N:26]([CH3:27])[C:24]1[C:23]([CH3:32])=[CH:22][C:17]2[NH:18][C:19](=[O:21])[CH2:20][C:14]([C:10]3[CH:11]=[CH:12][CH:13]=[C:8]([N:7]4[C:3]([CH2:4][N:5]5[CH2:39][CH2:40][CH2:41][CH2:42]5)=[N:44][CH:43]=[N:6]4)[CH:9]=3)=[N:15][C:16]=2[CH:25]=1)[CH:29]([CH3:31])[CH3:30]

参加物

7

反応物 5

HCID 312ChlorideHCID 6228DimethylformamideHCID 24386Thionyl ChlorideHCID 31268PyrrolidineHCID 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 186133567-(Isobutyl-methyl-amino)-8-methyl-4-[3-(5-pyrrolidin-1-ylmethyl-[1,2,4]triazol-1-yl)-phenyl]-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 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) (180 mg, 0.42 mmol) by reaction with thionylchloride in dichloromethane and subsequent treatment of the corresponding chloride with pyrrolidine in DMF according to the method described in Example 45. Obtained as an off-white solid (106 mg, 52%).

出典と根拠

ORDレコード
ord-8e98b3492e7e4a8496ceeb06f453bd0b
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…