2-Thiophenemethanol → 5-Fluoro-1-(2-thienylmethyl)pyrimidin-2-one

Participants

Reaction Conditions

Reaction Steps

N,N-Dimethylformamide dineopentyl acetal (1.76 ml) was added to a stirred suspension of 5-fluoropyrimidin-2-one (456 mg) and 2-hydroxymethyl thiophene (0.7 ml) in dry N,N-dimethylformamide (8 ml) under nitrogen and the mixture was then heated at 80° C. After 1 h the reaction mixture was evaporated to a brown solid which was crystallised twice from ethyl acetate to give white crystals of the title pyrimidinone (230 mg), m.p. 161°-163° C., λmax (EtOH) 222.5 nm (ε 10,890), 333.5 nm (ε 3,660).

Provenance & Evidence