Jiao Ping
2001
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Journal
Chinese Journal of Pharmaceuticals
Abstract
The synthesis of enadoline, a potent kappa opioid receptor agonist with high affinity and selectivity is described. The key intermediate,1 [8 methylamino 1 oxaspiro[4.5]dec 7 yl]pyrrolidine(16) was prepared from 1, 4 cyclohexadione via condensation, spirocyclization, reduction, epoxidation, the epoxy ring was opened with methylamine to give a mixture of aminoethanols followed by ring closure and then cleavage. 16 was acylated with 4 benzofuranacetic acid in the presence of the coupling agent CDI to form enadoline.