Cyclopropanecarboxaldehyde → HCID 131727397, compound

Participants

Reaction Steps

To a solution of 2-(4-fluorobenzyl)-8,9-dihydroxy-7-(piperidin-3-ylmethyl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione mono TFA salt (50 mg, 0.097 mmol) in anhydrous methanol (2 mL) under nitrogen, cyclopropanecarboxaldehyde (9 μL, 0.116mmol) was added and the solution was stirred at room temperature for one hour. Sodium cyanoborohydride (8 mg, 0.129 mmol) was added and the solution was stirred for another hour. The reaction mixture was concentrated under vacuum and the residue was purified by prep “HPLC [Gilson semi preparative HPLC system using a Waters Nova Pak column (10×40 mm I.D. cartridge, C18, 6 μM pore size) eluting with 95-5% water (0.10% TFA)/acetonitrile (0.10% TFA) gradient at 35 mL/min]. The product fractions were collected and lyophilized to provide the title compound as white solid.

Provenance & Evidence