The synthesis of Org-6370 is carried out in eight steps as follows: The 5,9-methanobenzocyclooctene system is prepared from tetralonepyrrolidine enamine (I) and acrolein (II), giving a mixture of the epimeric 8-alcohols (III), which are dehydroxylated via the intermediate p-toluenesulfonate esters. The unsaturated 11-ketone (IV) is converted by a reductive amination process using methylamine and sodium borohydride to an epimeric mixture of 11-methylamines. At this stage the epimeric amines are separated by crystallization and the required (11S*)-compound (V) is further methylated and converted to the hydrochloride.

The synthesis of Org-6370 is carried out in eight steps as follows: The 5,9-methanobenzocyclooctene system is prepared from tetralonepyrrolidine enamine (I) and acrolein (II), giving a mixture of the epimeric 8-alcohols (III), which are dehydroxylated via the intermediate p-toluenesulfonate esters. The unsaturated 11-ketone (IV) is converted by a reductive amination process using methylamine and sodium borohydride to an epimeric mixture of 11-methylamines. At this stage the epimeric amines are separated by crystallization and the required (11S*)-compound (V) is further methylated and converted to the hydrochloride.