In efforts aimed at further exploration of our finding that functional
ization of the two-carbon bridge of cocaine can lead to a weak antagon
ist of cocaine, we report a route to the 6- and 7-hydroxylated analogu
es by use of the Willstatter synthesis. The hydroxylated derivatives c
an in principle be used to gain access to a diverse library of 6- and
7-functionalized cocaine analogues. Copyright (C) 1996 Elsevier Scienc
e Ltd