Pyridine → US9296747, Example 2

Participants

Reaction Steps

A solution of N-(3,4,5-Trimethoxyphenyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-2-amine, Intermediate 1 (75 mg, 0.24 mmol) in CH2Cl2 (1.5 mL) was cooled to 0° C. and treated with benzoic anhydride (56.7 mg, 0.251 mmol) and pyridine (22 microliter, 0.273 mmol). After 1 hour the reaction mixture was diluted with CH2Cl2 and washed with water. The organic phase was collected, dried and concentrated. The residue was purified by silica gel chromatography (15-40% acetone/CH2Cl2). The product containing fractions were concentrated to give the title compound (75 mg).

Provenance & Evidence