反应详情

0.25 mmoles of the carboxylic acid of choice (2,5-difluorophenyl-acetic acid; 0.25 mmoles) and 0.25 mmoles of HBTU were dissolved in 1 mL amine-free DMF. To this solution was added dropwise a solution of 4-Amino-3-(4-aminophenyl)thieno[2,3-d]-pyrimidine in 1 mL DMF. The resulting solution was treated with 0.3 mL of Hunig's base. The system was stirred at room temperature overnight and then treated with 0.5 mL of 1:1 MeOH-diethylamine. The system was concentrated to dryness in a Speedvac system, reconstituted in 1 mL DMSO and purified by prep HPLC. MH+=397.

1. concentrationThe system was concentrated to dryness in a Speedvac system
2. custompurified by prep HPLC