反应详情

A mixture of 2-chloropyrimidine-5-carboxylic acid (2.00 g), ethyldiisopropylamine (6.39 mL), and chloro-N,N,N′,N′-tetramethylformamidinium hexafluorophosphate (4.21 g) in tetrahydrofuran (15 mL) is stirred for 45 min at room temperature prior to the addition of 4-cyclopropylamino-piperidine-1-carboxylic acid tert-butyl ester (2.94 g). The resulting mixture is stirred at room temperature for 1 h. The solvent is evaporated in vacuo and the residue purified by HPLC(H2O/MeOH/TFA). LC (method 3): tR=1.89 min; Mass spectrum (ESI+): m/z=381/383 (Cl) [M+H]+.

1. stirringThe resulting mixture is stirred at room temperature for 1 h
2. customThe solvent is evaporated in vacuo
3. customthe residue purified by HPLC(H2O/MeOH/TFA)