To obtain a new benzoxathionine derivative which is represented by a specific formula, has excellent physiological activity and is useful as an inhibitor of angiotensin converting enzyme or an acid secretion inhibitor.
The objective compound is represented by formula I (R is a 1-5C alkoxy, a perfluoroalkyl or an alkyl), preferably 3,4,6,7tetrahydro-1H-5,2- benzoxathionine. This compound is prepared, for example, by allowing phenylmagnesium bromide of formula H to react with 3-chloro-1,4-oxathiane of formula III in a mixed solvent of ether and/or toluene at 0-20°C for about 20 hours, then converting the product into a sulfonium salt using a trimethylsilylmethyl triflate, dissolving the product in DMSO and allowing the product to react with DBU or cesium fluoride.
SHIRAI NAOHIRO
SATO YOSHIRO
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