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Novel Method for Synthesis of Diarylpyrazole Derivatives as Cannabinoid CB1 Receptor Antagonists

机译:合成大麻素CB1受体拮抗剂的二芳基吡唑衍生物的新方法

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摘要

A novel and efficient method was developed for the synthesis of diarylpyrazole derivatives as cannabinoid CB1 receptor antagonist via four step reactions. The key step was the synthesis of a diarylpyrazole skeleton, which involved initial condensation of the sodium salt of compound 12 with diazonium compounds, and further cyclization by heating at reflux in acetic acid. Eight diarylpyrazole derivatives and nine new synthesized compounds were characterized by 1H NMR, IR, MS, and elemental analysis. The reaction conditions were mild and the overall yields of the target compounds ranged from 26% to 44%.

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