| 摘要 |
PROBLEM TO BE SOLVED: 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. SOLUTION: 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 R<1> 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 R<2> act on the A1 is subjected to optical resolution followed by conducting an N- fluorination. |
