A new process has been developed for the synthesis of optionally substituted 1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-ones. In particular, the process is particularly adaptable for the preparation of the 5,6-disubstituted compounds, e.g., 5,6-dimethyl-1,2,3,5-tetrahydroimidazo-[2,1-b]quinazolin-2-one. The compounds so prepared are useful as blood platelet anti-aggregative and/or antihypertensive agents in mammals, including humans.
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