We here present a simple and efficient method for the preparation of 2-substituted-thiazolomorphinanedienes 3-5. A protocol is also presented for yielding 3-demethoxy-14β-hydroxy derivatives of the thiazolomorphianedienes. The amino-, methyl- and phenyl-substituents connected in these compounds in a less rigid way to the “spacer” which offers the opportunity to test the effect of this sterically more flexible structure on the activity to opioid receptor subtypes.
Keywords: Hantzsch-type thiazole synthesis, morphinanediene, O-demethylation, introduction of 14-hydroxyl-motif
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