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Letters in Organic Chemistry

Author(s): Sultan Pathan, Anil Repale and Girdhar Pal *

DOI: 10.2174/1570178617666200207110526

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In-Situ Synthesis of Active Pharmaceutical Ingredients Which Content Pyrazole Skeleton

Page: [743 - 748] Pages: 6

  • * (Excluding Mailing and Handling)

Abstract

Celecoxib containing pyrazole derivatives were synthesized by path aldol condensation of substituted ketone with trifluoroethyl acetate subsequently by cyclization of the formed chalcones with 4-methanesulfonylphenylhydrazine. Here, a one-pot synthesis of celecoxib and substituted analogues have been reported which are nonsteroidal anti-inflammatory drugs for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. In order to intermediate work-up, a continuous one-pot synthesis has been developed, performing the entire reaction sequence that results in a shorter time with good yield.

Keywords: Pyrazoles, Claisen condensation, Cyclization, API, COX-1, COX-2.

Graphical Abstract

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