Abstract:
In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4"-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.
Abstract:
In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4''-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.
Abstract:
In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4''-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.
Abstract:
In one aspect, the invention relates to a process for preparing 6-O- substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4"-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates t o processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.
Abstract:
Preparation of 6-O-methylerythromycin A crystal form II comprising: (a) converting erythromycin A to 6-O-methylerythromycin A; (b) treating 6-O-methylerythromycin A with a solvent selected from (i) an 1-5C alkanol (except ethanol or isopropanol), (ii) a 5-12C hydrocarbon, (iii) a 3-12C ketone, (iv) a 3-12C carboxylic ester (except isopropyl acetate), (v) a 4-10C ether, (vi) benzene (optionally substituted by one or more substituents selected from 1-4C alkyl, 1-4C alkoxy, nitro or halo), (vii) a polar aprotic solvent, (viii) a compound of formula HNR1R2 where R1, R2 = H or 1-4C alkyl (provided that R1 and R2 are not both H), (ix) water and a water miscible solvent selected from a water miscible organic solvent and a water miscible alkanol, (x) methanol and a second solvent selected from a 5-12C hydrocarbon, a 2-5C alkanol, a 3-12C ketone, a 3-12C carboxylic ester, a 4-10C ether, benzene (optionally substituted by one or more substituents selected from 1-4C alkyl, 1-4C alkoxy, nitro or halo), (xi) a 5-12C hydrocarbon, a 3-12C carboxylic ester, a 4-10C ether of from 4 to 10 carbon atoms, benzene (optionally substituted by one or more substituents selected from 1-4C alkyl, 1-4C alkoxy, nitro or halo), and a polar aprotic solvent; and (c) isolating the 6-O-methylerythromycin A form II crystals.
Abstract:
In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4''-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.
Abstract:
In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4''-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.
Abstract:
In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4''-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.