Diisopropylethylamine → HCID 86656929、化合物

HRID 411012

反応式

HRID 411012 の反応式
Cl.Cl.[NH:3]1[CH2:7][CH2:6][CH:5]([NH:8][C:9]([C:11]2[CH:35]=[CH:34][C:14]3[N:15]([CH3:33])[C:16]([NH:18][C:19]4[S:20][C:21]5[CH:27]=[C:26]([O:28][C:29]([F:32])([F:31])[F:30])[CH:25]=[CH:24][C:22]=5[N:23]=4)=[N:17][C:13]=3[CH:12]=2)=[O:10])[CH2:4]1.[CH3:36][C@@H:37]1[CH2:39][O:38]1.CCN(C(C)C)C(C)C>CN(C=O)C.CO.C(Cl)Cl>[OH:38][C@H:37]([CH3:39])[CH2:36][N:3]1[CH2:7][CH2:6][CH:5]([NH:8][C:9]([C:11]2[CH:35]=[CH:34][C:14]3[N:15]([CH3:33])[C:16]([NH:18][C:19]4[S:20][C:21]5[CH:27]=[C:26]([O:28][C:29]([F:30])([F:31])[F:32])[CH:25]=[CH:24][C:22]=5[N:23]=4)=[N:17][C:13]=3[CH:12]=2)=[O:10])[CH2:4]1

参加物

7

反応物 3

HCID 81531DiisopropylethylamineHCID 146261(R)-1,2-EpoxypropaneHCID 86656927HCID 86656927、化合物

生成物 1

HCID 86656929HCID 86656929、化合物

試薬・触媒・溶媒 3

HCID 887Methanol溶媒HCID 6228Dimethylformamide溶媒HCID 6344Dichloromethane溶媒2 回

反応条件

温度
80 °C

実験手順

1-Methyl-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid [1-((R)-2-hydroxy-propyl)-pyrrolidin-3-yl]-amide (15 mg) was prepared using 1-methyl-2-(6-trifluoromethoxy-benzothiazol-2-ylamino)-1H-benzoimidazole-5-carboxylic acid pyrrolidin-3-ylamide dihydrochloride (47 mg), (R)-2-methyl-oxirane (excess) and DIEA (35 uL) in DMF (1 mL). The reaction was stirred at 80° C. overnight. The pure product was isolated through silica gel chromatography using DCM: (10%) methanol in DCM (from 100:0 to 0:100) as eluent system. LC/MS: m/z 534.6.

後処理

  1. customThe pure product was isolated through silica gel chromatography

出典と根拠

ORDレコード
ord-e1f688eda6b845e2906160ec3e7c79a8
出典データセット
uspto-grants-2014_06
特許番号
US08759535B2

関連ノート

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