Prepn. of psychotropic drug intermediates - from 3-nitro-4-amino:anisole by five-stage process to 2-methoxy-4-amino-5-alkyl sulphonyl:benzoic acids

摘要

Prepn. of 3-methoxy-4-amino-5- alkylsulphonylbenzoic acids of formula (I) by redn. of 3-nitro-4-alkylsulphonylanisole (A) (where R2 is 1-3C alkyl) to the 3-amino analogue (B), bromination of (B) to give 2-methoxy-4-amino-5alkyl -sulphonylbromobenzene (C), treating (C) with Cu2(CN2) to give 2-methoxy-4-amino-5 alkylsulphonylbenzonitrile (II) and hydrolysing. Cpd. (I) is as (II) with CN replaced by -CO2H. Cpds. A, B, C and (II) are new.