Diisopropylethylamine → 5-Methyl-2-{4-[(R)-1-(2-methyl-pyrimidin-5-yl)-ethylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-benzonitrile

Participants

Reaction Steps

A reaction mixture of 2-(4-chloro-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)-5-methylbenzonitrile (350 mg, 1.23 mmol) and (R)-1-(2-methylpyrimidin-5-yl)ethanamine (300 mg, 2.19 mmol) in acetonitrile (3 mL) and N,N-diisopropylethylamine (0.86 mL, 4.9 mmol) was subjected to microwave irradiation at 185° C. for 3.5 h. The reaction mixture was concentrated and the residue was purified by semi-preparative HPLC (100×20.2 mm, C18 column; 30-55% acetonitrile-water [10 mM Et2NH]) to yield an off-white solid.

Provenance & Evidence