A concise [C+NC+CC] coupling-enabled synthesis of kaitocephalinThis paper is dedicated to Professor Yasufumi Ohfune on the occasion of his retirement from Osaka City University.Electronic supplementary information (ESI) available: Experimental procedures and characterization data for all new compounds are provided. See DOI: 10.1039/c4cc01692k

A 15-step synthesis of the iGluR antagonist kaitocephalin from aspartic acid is reported. The linchpin pyrrolidine ring of the target molecule is efficiently assembled with in a single operation via an asymmetric [C+NC+CC] reaction. An efficient synthesis of the iGluR antagonist kaitocephalin is reported, employing an asymmetric [C+NC+CC] reaction in the key step.