Toluene → 6-bromo-3-[(1S,2S)-2-hydroxycyclohexyl]-10-methyl-7,8,9,10-tetrahydropyrido[3,2-h]quinazolin-4(3H)-one

Participants

Reaction Steps

A solution of 8-amino-5-bromo-N-[(1S,2S)-2-hydroxycyclohexyl]-1-methyl-1,2,3,4-tetrahydroquinoline-7-carboxamide (758 mg, 1.98 mmol) in toluene (6 mL) and DMF-DMA (5.3 mL) was heated in a sealed tube at 135° C. for 3 h. The resulting mixture was concentrated and purified by silica gel chromatography (0-4% MeOH/CH2Cl2) to afford 6-bromo-3-[(1S,2S)-2-hydroxycyclohexyl]-10-methyl-7,8,9,10-tetrahydropyrido[3,2-h]quinazolin-4(3H)-one in pure form.

Provenance & Evidence