To obtain a new optically active 1,2-benzisothiazole-1,1-dioxide derivative excellent in selectivity and reaction characteristics, and useful as the subject reagent to be used in the field of organic synthetic chemistry including medicine development.
This new compound is expressed by the formula [R1 and R2 differ from each other, being each H, a 1-10C (cyclic) alkyl, alkenyl, alkynyl, (substituted) phenyl, aryl or (substituted) aralkyl], e.g. (+)-2-fluoro-3-methy1-3- isopropyl-2,3-dihydro-1,2-benzisothiazole-1,1-dioxide. This compound is obtained by the following process: an alkyl Grignard reagent corresponding to R1 is made to act on saccharin to produce the corresponding imine form (A1); subsequently, the corresponding racemic form produced either by hydrogenating the A1 or by making an alkyl Grignard reagent corresponding to R2 act on the A1 is subjected to optical resolution followed by conducting an N- fluorination.
KOIZUMI TORU
SUZUKI TAKANORI
SATO AKIRA
KONNO KATSUHIKO
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