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- W2949662801 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 excellent regioselectivity and stereoselectivity. Process improvements and optimization of each step permitted elimination of column chromatography, resulting in a straightforward, practical synthesis of FK453." @default.
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- W2949662801 date "1999-09-03" @default.
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- W2949662801 title "Process Development of a Novel Non-Xanthine Adenosine A<sub>1</sub> Receptor Antagonist" @default.
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- W2949662801 doi "https://doi.org/10.1021/op990044w" @default.
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