反应详情

温度

50 °C

Intermediate 17 (350 mg, 0.63 mmol) and cyclopropyl-methylamine (45 mg, 0.63 mmol) were coupled using the procedure described in example 1; 1.9), where only 25% conversion of starting materials was discovered. Heating to 50° C. did not lead to further conversion. Then TOTU (246 mg, 0.75 mmol) was added and after stirring for 1 h at RT conversion was completed. The mixture was purified by preparative HPLC. Yield after lyophilization: 162 mg, 43%, colorless, amorphous solid.

1. customThe mixture was purified by preparative HPLC
2. customYield after lyophilization