Реакция #2366788

Уравнение реакции

28

N-(tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-amine

428

trans-(±)-4-(4-chloro-3-fluorophenoxy)-1-methylpyrrolidin-3-amine

CDI

→

2-(tetrahydro-pyran-4-ylamino)-5,8-dihydro-6H-pyrido[3,4-d]pyrimidine-7-carboxylic acid [4-(4-chloro-3-fluoro-phenoxy)-1-methyl-pyrrolidin-3-yl]-amide

Растворители

DCM

Условия реакции

Обработка

1. 1
   workup.STIRRINGThe reaction was stirred at RT for 2 h
2. 2
   ДругоеThe solvent was removed in vacuo
3. 3
   Другоеthe residue was purified by preparative reverse HPLC
4. 4
   Другоеto afford 31 mg (28%) of I-151 as a white solid

Методика

To a solution of 428 (0.085 g, 0.347 mmol) and DCM (15 mL) was added TEA (1 mL) and CDI (0.149 g, 0.919 mmol). The mixture was stirred at RT for 1 h and then 28 (0.081 g, 0.35 mmol) was added. The reaction was stirred at RT for 2 h. The solvent was removed in vacuo and the residue was purified by preparative reverse HPLC to afford 31 mg (28%) of I-151 as a white solid: LC-MS (ESI) m/z 505 (M+H).

Источник