Process development and scale-up of the PPAR agonist NNC 61-4655

…, B Weber, V Weil, SJ Mozer, P Sauerberg

Index: Deussen, Heinz-Josef; Jeppesen, Lone; Schaerer, Norbert; Junager, Finn; Bentzen, Bjorn; Weber, Beat; Weil, Volker; Mozer, Sandor Josef; Sauerberg, Per Organic Process Research and Development, 2004 , vol. 8, # 3 p. 363 - 371

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Citation Number: 24

Abstract

A scalable synthetic route of the nonselective but PPARα-preferring potent PPAR agonist NNC 61-4655 aimed for treatment of type 2 diabetes was developed. The synthetic pathway comprises the convergent synthesis and coupling of the two key intermediates E-5- (chloropent-3-en-1-ynyl) benzene 8 (prepared in a five-step synthesis in 18% overall yield) and (S)-2-ethoxy-3-(4-hydroxyphenyl) propanoic acid isopropyl ester 9. The 2- ...

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