Green Synthesis and Optimization of Celecoxib Catalyzed by Micro-nanometer Potassium Carbonate

FENG Juan, FU Wenna, WANG Jingkun, WANG Cuicui, LIU Shouxin

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主办:上海医药工业研究院
   中国药学会
   中国化学制药工业协会
ISSN 1001-8255   CN 31-1243/R   ZYGZEA
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Chinese Journal of Pharmaceuticals ›› 2024, Vol. 55 ›› Issue (12) : 1646-1650. DOI: 10.16522/j.cnki.cjph.2024.12.007
Paper

Green Synthesis and Optimization of Celecoxib Catalyzed by Micro-nanometer Potassium Carbonate

  • FENG Juan, FU Wenna, WANG Jingkun, WANG Cuicui, LIU Shouxin*
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Abstract

A green and efficient synthetic method of non-steroidal anti-inflammatory drug celecoxib(1) was reported in this paper. With p-methylacetophenone(2) and ethyl trifluoroacetate(3) as starting materials, the Claisen condensation was performed with potassium carbonate(98 nm) instead of sodium ethoxide by “one-pot method”. After the Claisen condensation and filtration, the filtrate without purification was cyclized with 4-hydrazinobenzene-1-sulfonamide hydrochloride(5) to obtain the target product 1. The total yield of celecoxib was 86.8% with HPLC purity of 99.65% . The alkali could be recovered by filtration and calcination, and its reuse had little effect on the yield. This green synthetic method has mild conditions, simple operation, short reaction period, good economy, high yield and less environmental pollution, which is suitable for industrial production.

Key words

celecoxib / green synthesis / Claisen condensation / micro-nanometer potassium carbonate / “one-pot method”

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FENG Juan, FU Wenna, WANG Jingkun, WANG Cuicui, LIU Shouxin. Green Synthesis and Optimization of Celecoxib Catalyzed by Micro-nanometer Potassium Carbonate. Chinese Journal of Pharmaceuticals. 2024, 55(12): 1646-1650 https://doi.org/10.16522/j.cnki.cjph.2024.12.007

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