| 摘要 |
<p>The derivs. of formula (I), in which n is 0, 1 or 2, and Y is Cl or F, are made by (a) treating 3-chloro or 3-fluoro 4-fluoro aniline with KCNS and bromine; (b) treating the prod. with NaOH to obtain the disulphide; (c) reacting the 1-bromo 2-chloro ethane to give 7-fluoro 8-chloro (or fluoro) 3,4-dihydro-2H 1,4-benzothiazine (II); (d) ring closure by reaction with ethyl ethoxy-methylene malonate at 80-160 deg.C and polyphosphoric acid; (e) hydrolysis and oxidn. to sulphoxide with H2O2; (f) nucleophilic substitn. with an amine of piperazine type in polar aprotic solvent at 70-160 deg.C; and (g) final redn.</p> |
