Practical and scalable synthesis of S1P1 receptor agonist ACT-209905

G Schmidt, S Reber, MH Bolli…

Index: Schmidt, Gunther; Reber, Stefan; Bolli, Martin H.; Abele, Stefan Organic Process Research and Development, 2012 , vol. 16, # 4 p. 595 - 604

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Citation Number: 9

Abstract

A practical and scalable route for the fast delivery of 12 kg of S1P1 agonist (ACT-209905) has been developed. ACT-209905 is composed of an amino pyridine group, an oxadiazole spacer, a 2-ethyl-5-methylphenol moiety and a chiral 1-amino-2-propanol side chain. The convergent synthesis consists of 16 steps with 9 isolated intermediates and is chromatography-free. Key building blocks are accessed from low-cost starting materials, ...