反应详情

2-Chloro-9-cyclopentyl-7,7-difluoro-5-methyl-8,9-dihydro-5H-pyrimido[5,4-b][1,4]diazepin-6(7H)-one (obtained above), 4-amino-3-methoxy benzoic acid (334 mg, 2 mmol), i-PrOH (10 mL) and conc. HCl (10 drops) were heated to 100° C. overnight. The reaction mixture was then cooled to room temperature, concentrated and redissolved in MeOH, treated with NaOH and refluxed for 1 hr. After which, it was concentrated, acidified with HCl and filtered to give the title as a tan solid (300 mg). [M+H] calc'd for C21H23F2N5O4, 448; found 448.

1. concentrationconcentrated
2. dissolutionredissolved in MeOH
3. additiontreated with NaOH
4. temperaturerefluxed for 1 hr
5. concentrationAfter which, it was concentrated
6. filtrationfiltered