US 2010/0145035 A1 · METHOD OF SYNTHESIZING MACROLIDE COMPOUNDS

Abstract

The present invention relates to methods for synthesizing macrolide compounds which are known to have antibacterial activity, and are useful in the therapy of bacterial infections in mammals. More specifically, the invention relates to methods for synthesizing the macrolide antibiotic, gamithromycin utilizing a novel configuration of catalysts, chemical structures, and/or methods. An embodiment of the present invention may include allowing multiple chemical reactions to proceed without the isolation of chemical intermediates. Thus, multiple reactions may occur in one reaction vessel allowing for a considerable decrease in the cycle-time. The present invention also provides a novel method for inhibiting degradation while isolating a structure of a pharmaceutical composition.

Claims16

Dependent claims

A process for synthesizing a macrolide compound comprising:

(i) converting a compound of structure 2 to a compound of structure 3;
(ii) reducing the compound of structure 3 in the presence of a polar aprotic solvent and a reducing agent to form a compound of structure 7;
and
(iii) reacting the compound of structure 7 with an aldehyde of structure R—C(O)H in the presence of a reducing agent to form a compound of Structure 8a;
wherein R is hydrogen, alkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl;
and.

3 more elements

Dependencies are inferred from the claim text.

Method of synthesizing macrolide compounds

Life of this patent

Method of synthesizing macrolide compounds

Life of this patent

Abstract

Claims16