2-氨基吡啶置于盐酸,硫酸,三氧化硫,溴,Sodium Nitrite体系中,用 水 用作溶剂,化学反应 9.5H,反应生成3-溴-2-氯吡啶-5-磺酰氯
参考文献:The Discovery Of Uk-369003,A Novel Pde5 Inhibitor With The Potential For Oral Bioavailability And Dose-Proportional Pharmacokinetics
标题:The Discovery Of Uk-369003,A Novel Pde5 Inhibitor With The Potential For Oral Bioavailability And Dose-Proportional Pharmacokinetics
摘要:This Paper Describes Our Recent Efforts To Design And Synthesise Potent And Selective Pde5 Inhibitors And The Use Of In Vitro Predictors Of Clearance,Absorption And Permeability To Maximise The Potential For Dose-Proportional Pharmacokinetics And Good Oral Bioavailability In Man. Optimisation Of The Preclinical Profile Resulted In The Identification Of Uk-369003 (19A) And Its Nomination As A Clinical Candidate. The Clinical Pharmacokinetic And Safety Profile Has Enabled Us To Progress The Compound To Test Its Efficacy In Patients With Lower Urinary Tract Symptoms (Luts) Associated With Benign Prostatic Hyperplasia (Bph) And A Paper Describing Its Efficacy Has Recently Been Published. 2,3 (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2011.10.022