Hydrochloric Acid → 4H-Pyrido[1,2-a]pyrimidin-4-one, 3-(2-chloroethyl)-9-hydroxy-2-methyl-, hydrochloride

Participants

Reaction Conditions

Reaction Steps

A mixture of 3-benzyloxy-2-aminopyridine (formula-2) (100 grams), toluene (3.5 L) and phosphorusoxychloride (139 ml) was heated to 50° C. 3-acetyldihydrofuran-2(3H)-2-one (218 grams) (formula-3) was added to the reaction mixture, heated to 95° C. and stirred for 18 hrs. The solvent was distilled off under reduced pressure to obtain a residue which was cooled to 40° C. and toluene (500 ml) was added to it. A solution of concentrated hydrochloric acid (600 ml) was added to the reaction mixture, heated to 60° C. and stirred for 6 hrs. The reaction mixture was cooled to 0° C. A solid crystallized out which was filtered, washed with toluene and dried at 50° C. to yield the title compound.

Provenance & Evidence