Synthesis of the 6- and 7-hydroxylated cocaines and pseudococaines

Article abstract of DOI:10.1016/0040-4039(96)01123-9

In efforts aimed at further exploration of our finding that functionalization of the two-carbon bridge of cocaine can lead to a weak antagonist of cocaine, we report a route of the 6- and 7-hydroxylated analogues by use of the Willstatter synthesis. The hydroxylated derivatives can in principle be used to gain access to a diverse library of 6- and 7-functionalized cocaine analogues.