反应详情

Under an atmosphere of argon protective gas, (7R)-2-amino-7-(4-cyanophenyl)-5-methyl-4-[3-(trifluoromethyl)phenyl]-4,7-dihydro[1,2,4]triazolo[1,5-a]pyrimidine-6-carbonitrile hydrochloride (13 mg, 28 mmol) was dissolved in abs. pyridine (0.65 ml). At room temperature, cyclohexanecarbonyl chloride (8.3 mg, 57 mmol, 2 eq.) was added. After 12 h, analysis of the reaction by HPLC showed substantial conversion. The reaction mixture was concentrated under reduced pressure and purified by preparative HPLC (Kromasil C18 column, 20×50 mm; mobile phase: acetonitrile-water-0.1% TFA). After lyophilization, the product was obtained as a solid (12.5 mg, 83% of theory).

1. customanalysis of the reaction by HPLC
2. concentrationThe reaction mixture was concentrated under reduced pressure
3. custompurified by preparative HPLC (Kromasil C18 column, 20×50 mm; mobile phase: acetonitrile-water-0.1% TFA)
4. customAfter lyophilization, the product was obtained as a solid (12.5 mg, 83% of theory)