| 摘要 |
<p>A process for the preparation of substituted benzothiazinoindoles of general formula (I) wherein R<SUB>1</SUB>, R<SUB>2</SUB>, and R<SUB>4 </SUB>are independently selected from hydrogen, chloro, fluoro, amino, nitro, cyano, CHO, (C<SUB>1</SUB>-C<SUB>3</SUB>)alkyl, perhalo(C<SUB>1</SUB>-C<SUB>3</SUB>)alkyl, (C<SUB>1</SUB>-C<SUB>3</SUB>)alkoxy, aryl, aralkyl, aralkoxy, (C<SUB>5</SUB>-C<SUB>7</SUB>)heterocyclyl, (C<SUB>5</SUB>-C<SUB>7</SUB>)heterocyclylalkyl, (C<SUB>5</SUB>-C<SUB>7</SUB>)heterocyclyloxy, acyl, acetyl, alkylamino, aminoalkyl, amide, hydroxyalkyl, carboxylic acid and its derivatives. The process comprises cyclization of compound of general formula-II (i.e. substituted 1-benzenesulfonyl-7-bromo-1H-indole), formula (II) wherein R<SUB>1</SUB>, R<SUB>2</SUB>, R<SUB>3 </SUB>and R<SUB>4 </SUB>are attached using suitable catalyst and solvents.</p> |
