CAS: 13451-78-0; 5-Fluorobenzo[d]Oxazole-2-Thiol

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📜2-硝基-4-氟苯酚置于sulfide Carbon,铂 氢氧化钾,氢气体系中,用 乙醇,乙酸乙酯 用作溶剂,化学反应 32.0H,反应生成5-氟苯并恶唑-2-硫醇
参考文献:Benzoxazole Derivatives As Novel 5-Ht3 Receptor Partial Agonists In The Gut
标题:Benzoxazole Derivatives As Novel 5-Ht3 Receptor Partial Agonists In The Gut
摘要:A Series Of Benzoxazoles With A Nitrogen-Containing Heterocyclic Substituent At The 2-Position Was Prepared And Evaluated For 5-Ht3 Partial Agonist Activity On Isolated Guinea Pig Ileum. The Nature Of The Substituent At The 5-Position Of The Benzoxazole Ring Affected The Potency For The 5-Ht3 Receptor,And The 5-Chloro Derivatives Showed Increased Potency And Lowered Intrinsic Activity. 5-Chloro-7-Methyl-2-(4-Methyl-1-Homopiperazinyl)Benzoxazole (6V) Exhibited A High Binding Affinity In The Same Range As That Of The 5-Ht3 Antagonist Granisetron,And Its Intrinsic Activity Was 12% Of That Of 5-Ht. Compound 6V Inhibited 5-Ht-Evoked Diarrhea But Did Not Prolong The Transition Time Of Glass Beads In The Normal Distal Colon Even At A Dose Of 100 Times The Ed50 For Diarrhea Inhibition In Mice. Compounds Of This Type Are Expected To Be Effective For The Treatment Of Irritable Bowel Syndrome Without The Side Effect Of Constipation.
Doi:10.1021/jm9801004