Thiazine-1,1-dioxide and isothiazole-1,1-dioxide derivatives and process for preparation

A method which comprises reacting (a) a compound of the formula ##STR37## wherein R.sup.0 is perhalomethyl selected from trifluoromethyl, difluoromethyl, difluorochloromethyl, dichlorofluoromethyl, dichloromethyl and trichloromethyl;

• R.sup.1 is hydrogen or perhalomethyl having the same meaning given above;
• R.sup.2 is hydrogen or methyl;
• R.sup.3 is hydrogen, alkyl or alkoxy;
• R.sup.2 and R.sup.3 taken together represent the carbon atoms necessary to complete a fused benzene ring;
• and (b) a compound of the formula ##STR38## wherein R.sup.4 and R.sup.6 each are hydrogen, alkyl, alkoxy, chloro or fluoro;
• R.sup.5 is hydrogen, alkyl, alkoxy, --OP.sup.I wherein P.sup.I is a protecting group, --N,N-(dialkyl)amino, --N,N-(w-R.sup.8 -alkyl).sub.2 --amino wherein R.sup.8 is halo or --OP.sup.II wherein P.sup.II is a protecting group;
• --NHCOCH.sub.3, piperidino, pyrrolidino, N-methylpiperazino, morpholino, thiomorpholino or tetrahydro-2H,4-H-1,3,6-dioxazocino;
• R.sup.7 is hydrogen, alkyl, alkoxy or --OP.sup.III wherein P.sup.III is a protecting group usually the same as P.sup.I or P.sup.II ;
• R.sup.6 and R.sup.7 taken together represent the carbon atoms necessary to complete a fused benzene ring provided R.sup.2 and R.sup.3 are taken separately when R.sup.6 and R.sup.7 are taken together;
• R.sup.4, R.sup.5 and R.sup.6 taken together represent the atoms necessary to complete a fused [ij]quinolizidine ring;
• and X' represents the atoms necessary to complete benz[d]isothiazole-1,1-dioxide or naphtho[1,8-de]-1,2-thiazine-1,1-dioxide in an inert organic solvent at a temperature between about -80.degree. C. and 50.degree. C. to give the corresponding reaction product and hydrolyzing said reaction product at pH 6 to give (c) the compound having the formula ##STR39## wherein R.sup.0, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the same meaning given above and X represents the atoms necessary to complete 2,3-dihydrobenz[d]isothiazole-1,1-dioxide or 2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxide.