CAS: 1393813-41-6; Potassium (N-Propylsulfamoyl)Amide

相似化合物

147962-41-2 92577-65-6 154743-01-8

丙胺基磺酰胺置于potassium Tert-Butylate体系中,用 甲醇 用作溶剂,化学反应 3.0H,以32.4 G的收率获得n-丙基-磺酰胺钾盐
参考文献:的发现ñ-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]-ñ '-Propylsulfamide(美西特田),一种口服活性,强效双重内皮素受体拮抗剂
标题:的发现ñ-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]-ñ '-Propylsulfamide(美西特田),一种口服活性,强效双重内皮素受体拮抗剂
摘要:从波生坦(1)的结构开始,我们着手于一项药物化学程序,旨在鉴定具有高口服功效的新型有效的双重内皮素受体拮抗剂.这导致发现了一系列新的烷基磺酰胺取代的嘧啶.其中,化合物17(macitentan,Act-064992)引起了人们的特别关注,因为它是对et B受体具有显着亲和力的et A的有效抑制剂,并且在高血压dahl盐敏感性大鼠中显示出优异的药代动力学特性和高体内功效.化合物17成功完成了一项肺动脉高压的长期iii期临床试验.
Doi:10.1021/jm3009103

专利信息

专利号:US-11667610-B2
优先权日:2016-09-28
标题:Method for preparing Macitentan and intermediate compound thereof
发明人：JIA QIANG; MA CHI; YANG ZHENGWEI; YANG JINJIN
权利人:SEASONS BIOTECHNOLOGY TAIZHOU CO LTD
摘要:The present invention relates to technical field of chemical synthesis of drugs, and provides a preparation method of Macitentan and intermediate compound thereof. Adding THF solution containing compound II and 5-bromo-2-chloropyrimidine slowly into THF solution containing base to react, or adding THF solution containing compound II and THF solution containing 5-bromo-2-chloropyrimidine slowly at the same time into THF solution containing base to react and obtain Macitentan (shown as compound I), wherein the base is selected from sodium hydride, potassium hydride, lithium hydride or lithium bis(trimethylsilyl)amide. The selectivity of the preparation method is very good, which is suitable for industrial production. The obtained product Macitentan has good quality and high yield. And the product compound II also has good quality and high yield, its HPLC purity is up to 99.0%, the content of impurity A is less than 0.20%, the content of impurity B is less than 0.25%.