Formaldehyde → HCID 73214394, compound

Participants

Reaction Steps

In THF (20 mL) was dissolved the above N-(7-azaspiro[3.5]nonan-2-ylmethyl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-((3-chloro-4-methoxybenzyl)amino)pyrimidine-5-formamide. Formalin (1 mL) was added. The reaction was conducted at ambient temperature for 1 h, sodium triacetoxyborohydride (134 mg, 0.63 mmol) was added and the reaction was continued for 4 h. The reaction was quenched with water. The reaction mixture was filtrated. The organic phase was dried and concentrated. The obtained solid was purified by silica gel column chromatography (DCM/methanol=20/1) to give 2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-((3-chloro-4-methoxybenzyl)amino)-N-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methyl) pyrimidine-5-formamide (39 mg, 21% yield).

Provenance & Evidence