Abstract:
PROBLEM TO BE SOLVED: To provide a method for preparing quinoline-substituted carbonate and carbamate compounds which are important intermediates in the synthesis of a 6-O-substituted macrolide antibiotic material. SOLUTION: The carbonate or carbamate derivative expressed by the formula: R 1 -CH=CHCH 2 OC(O)-X-R 2 (I) is obtained by coupling a haloquinoline with propargyl alcohol in the presence of a base and a palladium-based catalyst to form an alkynol, reducing it to make an alkenol and then reacting it with an acylation reagent. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.
Abstract:
The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors, comprising the reaction of 1-formyl indoline with clorosulfonic acid and thionyl chloride, followed by reaction with an aromatic amine.
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:
A compound of formula (I), or a pharmaceutically acceptable salt thereof, is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
Abstract:
The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or substrate that can be reduced to obtain the same.
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.