Processes and intermediates for the preparation of piperazine derivatives
申请人:John Wyeth & Brother Ltd.
公开号:US06133449A1
公开(公告)日:2000-10-17
Compounds having the formula R.sup.5 O--A--NR.sup.4 --R.sup.2 (V) where R.sup.2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R.sup.4 and R.sup.5 are both hydrogen atoms or together represent --SO-- or --SO.sub.2 -- and A is C.sub.2 -C.sub.4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R.sup.4 and R.sup.5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI). R.sup.2 O--A--NH.sub.2 (VI)
Compounds are disclosed which have the general formula A: ##STR1## where R.sup.a and R.sup.b are each hydrogen or methyl and R.sup.c is hydrogen, halo or C.sub.1-4 alkyl optionally in the form of a pharmaceutically acceptable acid addition salt. The compounds are useful in the treatment of CNS disorders.