Process for 6-O-alkylation of erythromycin derivatives

Details Process for 6-O-alkylation of erythromycin derivatives Process for 6-O-alkylation of erythromycin derivatives

2006-11-07

2006-11-07

Peselev, Elli (Department: 1623)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

C536S007200, C536S007300, C536S007400, C536S018500

Reissue Patent

active

RE039383

ABSTRACT:
A procedure for preparing 6-O-alkyl erythromycin compounds having the formula:wherein R1is a loweralkyl group, R2and R3an independently hydrogen or a hydroxy-protecting group, except that R2and R3may not both be hydrogen simultaneously; Y is oxygen or a specifically substituted oxime; and Z is hydrogen, hydroxy or protected-hydroxy; by reaction of the compound wherein R1is hydrogen with an alkylating reagent, is the presence of a strong alkali metal base and also in the presence of a weak organic amino base, in a suitable stirred or agitated polar aprotic solvent, or a mixture of such polar aprotic solvents maintained at a reaction temperature and for a period of time sufficient to effect alkyation.

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