Condensed Thienopyrimidines. I. : Synthesis and Gastric Antisecretory Activity of 2, 3-Dihydro-5H-oxazolothienopyrimidin-5-one Derivatives

Abstract

A practical preparation of various 2, 3-dihydro-5H-oxazolo[3, 2-a]thieno[3, 2-d]-, [3, 4-d]-, and [2, 3-d]pyrimidin-5-one derivatives was developed starting from the corresponding aminothiopheneesters in two steps, and their chloro-substituted derivatives were prepared. These compounds were evaluated for gastric antisecretory activity in pylorus-ligated rats, compared to the anti-ulcer standard, cimetidine, and their structure-activity relationships are discussed.