PROCESS FOR PREPARING BENZOTHIAZEPINES FROM .GAMMA.-AMINOALKYLBENZENES

摘要

The invention provides a process for preparing a 2,3,4,5--tetrahydro[1,4]benzothiazepine of formula: [I] by reacting a [2--(acylaminoethyl)thio]arene of formula [II] with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2--(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula [III]; then treating the [N--hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahy-dro[1,4]benzothiazepine.