The development of efficient methods for the catalytic asymmetric synthesis of stereogenic centres is one of the most vibrant and important fields of research in organic chemistry.  The need for a practical, cost-effective manufacturing route to a CGRP receptor antagonist in clinical trials inspired the discovery of new methodologies for the asymmetric synthesis of carbocyclic and heterocyclic ring systems. Highlights of these endeavors will be presented, with the development of novel phase-transfer catalysis (PTC) processes for the synthesis of spirocyclic oxindoles being discussed in detail.  The application of this chemistry to large scale production of the structurally complex drug candidate is also illustrated.

Development of an efficient asymmetric synthesis of a CGRP receptor antagonist

248th National Meeting (2014)

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