Process development of a novel non-xanthine adenosine A1 receptor antagonist

…, Y Morinaga, H Yasuda, H Yamazaki

Index: Zanka, Atsuhiko; Uematsu, Ryoichi; Morinaga, Yasuhiro; Yasuda, Hironobu; Yamazaki, Hiroshi Organic Process Research and Development, 1999 , vol. 3, # 6 p. 389 - 393

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Citation Number: 11

Abstract

(+)-(R)-1-[(E)-3-(2-phenylpyrazolo [1, 5-a] pyridin-3-yl) acryloyl]-2-piperidine ethanol (FK453) is a novel, potent adenosine A1 receptor antagonist for the regulation of renal function. The development of a reliable process suitable for large scale manufacture is described. A Horner-Emmons reaction and a 1, 3-dipolar cycloaddition were successfully scaled up to afford ethyl (E)-3-(2-phenylpyrazolo [1, 5-a] pyridin-3-yl) acryloylate, with ...