Hydrochloric Acid → HCID 57860920, compound

Participants

Reaction Steps

A mixture of 2-[2-(3-aminopropoxy)-4-(morpholin-4-yl)benzoylamino]-N-(5-chloropyridin-2-yl)-5-fluorobenzamide (400 mg, 0.76 mmol), paraformaldehyde (96 mg, 3.19 mmol) and MeOH (75 mL) was adjusted to pH 5-6 with AcOH. Sodium cyanoborohydride (96 mg, 1.57 mmol) was added. After stirring overnight, the reaction was acidified with 1 N HCl (pH=2) and stirred for 2 hours. Methylene chloride was added to the mixture and it was basified with 50% satd Na2 CO3. The organic layer was dried (Na2 SO4) and concentrated to give the desired product (418 mg, 99%).

Provenance & Evidence