📜5-甲基-噻吩并[2,3-D]嘧啶-2,4(1H,3H)-二酮置于n,N-二甲基苯胺,三氯氧磷体系中,化学反应 16.0H,以31%的收率获得产物2,4-二氯-5-甲基噻吩并[2,3-D]嘧啶
参考文献:The Highly Potent And Selective Dipeptidyl Peptidase Iv Inhibitors Bearing A Thienopyrimidine Scaffold Effectively Treat Type 2 Diabetes
标题:The Highly Potent And Selective Dipeptidyl Peptidase Iv Inhibitors Bearing A Thienopyrimidine Scaffold Effectively Treat Type 2 Diabetes
摘要:New Dipeptidyl Peptidase Iv Inhibitors Were Designed Based On Alogliptin Using A Scaffold-Hopping Strategy. All Of The Compounds Constructed On A Thienopyrimidine Scaffold Demonstrated Good Inhibition And Selectivity For Dpp-Iv. Compound 10D Exhibited Subnanomolar (Ic50 = 0.33 Nm) Dpp-Iv Inhibitory Activity,Good In Vivo Efficacy And An Acceptable Pharmacokinetic Profile. A Pharmacokinetic-Driven Optimization Of 10D May Lead To A New Class Of Clinical Candidate Dpp-Iv Inhibitors. (C) 2010 Elsevier Masson Sas. All Rights Reserved.
DOI:10.1016/j.Ejmech.2010.10.016