4-Methylmorpholine → N-(2-Amino-Pyrimidin-5-yl)-2-Chloro-5-(3-Trifluoromethyl-Benzoylamino)-Benzamide

HRID 1662834

反応式

HRID 1662834 の反応式
[F:1][C:2]([F:23])([F:22])[C:3]1[CH:4]=[C:5]([CH:19]=[CH:20][CH:21]=1)[C:6]([NH:8][C:9]1[CH:10]=[CH:11][C:12]([Cl:18])=[C:13]([CH:17]=1)[C:14](O)=[O:15])=[O:7].CN1CCOCC1.[NH2:31][C:32]1[N:37]=[CH:36][C:35]([NH2:38])=[CH:34][N:33]=1>C(Cl)Cl>[NH2:31][C:32]1[N:37]=[CH:36][C:35]([NH:38][C:14](=[O:15])[C:13]2[CH:17]=[C:9]([NH:8][C:6](=[O:7])[C:5]3[CH:19]=[CH:20][CH:21]=[C:3]([C:2]([F:22])([F:23])[F:1])[CH:4]=3)[CH:10]=[CH:11][C:12]=2[Cl:18])=[CH:34][N:33]=1

参加物

5

反応物 3

HCID 79724-MethylmorpholineHCID 229075Pyrimidine-2,5-diamineHCID 534011722-Chloro-5-(3-(trifluoromethyl)benzamido)benzoic acid

生成物 1

HCID 24962185N-(2-Amino-Pyrimidin-5-yl)-2-Chloro-5-(3-Trifluoromethyl-Benzoylamino)-Benzamide収率 73%

試薬・触媒・溶媒 1

HCID 6344Dichloromethane溶媒

実験手順

A solution of intermediate 1 (Example 2) (380 mg, 1.11 mmol) in DCM was charged with CDMT (233 mg, 1.33 mmol), and NMM (0.3 mL, 2.73 mmol). After 1 hr of stirring, 2,5-diaminopyrimidine (121 mg, 1.10 mmol) was added and the solution was allowed to stir for 48 h. The mixture was concentrated and purified by HPLC to afford the title compound as a white solid (350 mg, 73%).

後処理

  1. stirringto stir for 48 h
  2. concentrationThe mixture was concentrated
  3. custompurified by HPLC

出典と根拠

ORDレコード
ord-22c9db19a4fe4ff899c5f9e817647a15
出典データセット
uspto-grants-2011_10
特許番号
US08030487B2

関連ノート

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