ONE-POT NON-SYMMETRIC HETEROBIFUNCTIONAL COUPLING OF ORGANIC MOLECULES THROUGH MALONIC ACID DERIVATIVES

摘要

The present invention relates to a one-pot method for the chemoselective non-symmetrical coupling of two different organic molecules. The method involves coupling of a silyl-monoprotected dicarboxylic acid such as tert-butyldiphenylsilylmalonate and a first nucleophilic organic molecule in the presence of a coupling reagent such as a carbodiimide, deprotection of the silyl protecting group, and coupling with a second nucleophile in the presence of a second coupling reagent. The method is advantageously practiced in one pot, without the need to isolate and purify reaction intermediates.