Chloroacetaldehyde → HCID 178457306, compound

Participants

Reaction Steps

To a methanolic solution of 2-(1-amino-1-methylethyl)-N-(4-fluorobenzyl)-5,6-dihydroxypyrimidine-4-carboxamide hydrochloride (prepared as described in WO2003035076 A1) Et3N (1 eq.), chloroacetaldehyde (2 eq.), AcOH (ca. 1.5 eq.) were added and subsequently NaBH3CN (1.5 eq.). The reaction mixture was stirred at room temperature overnight. To drive the reaction to completion a few drops of TFA were added and stirring was prolonged for a further 1.5 hours. MeOH was removed under reduced pressure to yield the title amine as crude. MS (ES) C17H20ClFN4O3 requires 383. Found: 384 (M+H+).

Provenance & Evidence