📜2-氯-4-氟苯甲酸置于氯磺酸,Ammonium Hydroxide体系中,用 1,4-二氧六环,水 作为反应溶剂,化学反应生成 2-氯-4-氟-5-氨磺酰基苯甲酸
参考文献:Novel 4,4-Disubstituted Piperidine-Based C-c Chemokine Receptor-5 Inhibitors With High Potency Against Human Immunodeficiency Virus-1 And An Improved Human Ether-A-Go-Go Related Gene (Herg) Profile
标题:Novel 4,4-Disubstituted Piperidine-Based C-c Chemokine Receptor-5 Inhibitors With High Potency Against Human Immunodeficiency Virus-1 And An Improved Human Ether-A-Go-Go Related Gene (Herg) Profile
摘要:We Recently Described (J. Med. Chem. 2008,51,6538-6546) A Novel Class Of Ccr5 Antagonists With Strong Anti-Hiv Potency. Herein,We Detail Sar Converting Leads 1 And 2 To Druglike Molecules. The Pivotal Structural Motif Enabling This Transition Was The Secondary Sulfonamide Substituent. Further Fine-Tuning Of The Substituent Pattern In The Sulfonamide Paved The Way To Enhancing Potency And Bioavailability And Minimizing Herg Inhibition,Resulting In Discovery Of Clinical Compound 122 (Gsk163929).
DOI:10.1021/jm200279V