CAS: 1393813-43-8; N-(5-(4-Bromophenyl)-6-(2-Hydroxyethoxy)Pyrimidin-4-yl)Propane-1-Sulfamide

相似化合物

1393813-42-7 2365406-87-5 2365406-85-3

上下游产品

马西替坦 Macitentan 441798-33-0
N-[5-(4-溴苯基)-6-氯-4-嘧啶基]-N'-丙基氨基磺酰胺 N-5-(4-Bromophenyl)-6-Chloro-4-Pyrimidinyl-N'-Propylsulfamide 1393813-42-7

4-溴苯乙酸甲酯置于potassium Tert-Butylate,Sodium,Sodium Hydride,三氯氧磷体系中,用 四氢呋喃,甲醇,乙二醇二甲醚,二甲基亚砜,N,N-二甲基苯胺,Mineral Oil 用作溶剂,化学反应 171.17H,反应生成N-[5-(4-溴苯基)-6-(2-羟基乙氧基)-4-嘧啶基]-N'-丙基氨基磺酰胺
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%.