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

HRID 1662834

Reaktionsgleichung

Reaktionsgleichung von HRID 1662834
[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

Komponenten

5

Edukt 3

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

Produkt 1

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

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Versuchsvorschrift

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%).

Aufarbeitung

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

Quellen und Nachweise

ORD-Eintrag
ord-22c9db19a4fe4ff899c5f9e817647a15
Quelldatensatz
uspto-grants-2011_10
Patentnummer
US08030487B2

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