Chemical and pharmaceutical bulletin p. 1197 - 1200 (1989)
Update date:2022-08-28
Topics:
Fukumi
Sugiyama
Sakamoto
A practical preparation of 2,3-dihydro-5H-oxazolo[3,2-a]thieno[3,2-d]pyrimidin-5-one (2) from methyl 3-aminothiophene-2-carboxylate in two steps was developed. The addition reactions of various nucleophiles to 2 were investigated and oxazole-ring-opened compounds were produced (5, 6, 12, 13 and 14). Desulfurization reaction of 2 with Raney Ni gave an oxazolo[3,2-a]pyrimidine derivative (15). It was found that 2 showed potent anti-gastric secretion activity.
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Doi:10.1039/c39840000804
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