The Fit For Purpose Development of S1P1 Receptor Agonist GSK2263167 Using a Robinson Annulation and Saegusa Oxidation to Access an Advanced Phenol Intermediate

• Published in: Organic process research & development Vol. 17; no. 10; pp. 1239 - 1246
• Main Authors: Harris, Robert M, Andrews, Benjamin I, Clark, Stacy, Cooke, Jason W. B, Gray, John C. S, Ng, Stephanie Q. Q
• Format: Journal Article
• Language: English
• Published: American Chemical Society 18.10.2013

A fit for purpose approach has been adopted in order to develop a robust, scalable route to the S1P1 receptor agonist, GSK2263167. The key steps include a Robinson ring annulation followed by a Saegusa oxidation, providing rapid access to an advanced phenol intermediate. Despite the use of stoichiom...