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

HRID 1662834

반응식

HRID 1662834 반응식
[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

참가 물질

5

반응물 3

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

생성물 1

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

시약·촉매·용매 1

HCID 6344Dichloromethane용매

실험 절차

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%).

후처리

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

출처 및 근거

ORD 기록
ord-22c9db19a4fe4ff899c5f9e817647a15
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08030487B2

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