METHODS FOR MAKING 3-O-PROTECTED MORPHINONES AND 3-O-PROTECTED MORPHINONE DIENOL CARBOXYLATES

摘要

Disclosed are methods for making aldehydes and ketones comprising allowing the corresponding primary or secondary alcohol to react in the presence of trichoroisocyanuric acid, a compound of formula R1SR2 and a base. In one embodiment, the alcohol is a compound of formula (I):;;wherein R3 is a protecting group.;Also disclosed are methods for making 3-O-protected morphine dienol carboxylates comprising allowing a compound of formula (I) to oxidize in the presence of a chlorine-containing compound and a compound of formula R1SR2; and allowing the product of the oxidation step to react with an acylating agent.

主权项

1. A composition comprising trichloroisocyanuric acid, an alcohol selected from the group consisting of primary alcohols and secondary alcohols, a base, and a compound of formula R1SR2, wherein R1 and R2 are each independently —(C1-C20)alkyl, —(C3-C8)cycloalkyl, or -phenyl.