CAS: 1103522-45-7; N-(5-(4-Bromophenyl)-6-(2-((5-Bromopyrimidin-2-yl)Oxy)Ethoxy)Pyrimidin-4-yl)Sulfamide

上下游产品

Benzylsulfamic Acid {5-(4-Bromophenyl)-6-[2-(5-Bromopyrimidin-2-Yloxy)-Ethoxy]-Pyrimidine-4-Yl}-Amide 441796-09-4
N-[5-(4-Bromophenyl)-6-Chloro-4-Pyrimidinyl]-N'-Benzyl-Sulfamide 441797-42-8

5-(4-Bromophenyl)-4-(2-((5-Bromopyrimidin-2-yl)Oxy)Ethoxy)-6-Fluoropyrimidine置于potassium Carbonate,磺酰胺体系中,用 二甲基亚砜 用作溶剂,化学反应 3.0H,以84%的收率获得act 132577; N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺
参考文献: Process For Manufacturing Pyrimidine Sulfamide Derivatives[fr] Procédé De Fabrication De Dérivés De Pyrimidine Sulfonamide
标题: Process For Manufacturing Pyrimidine Sulfamide Derivatives[fr] Procédé De Fabrication De Dérivés De Pyrimidine Sulfonamide
摘要:本发明涉及一种制造式i化合物的过程,其中r为h,(C1-C6)烷基或苄基,或其盐,该过程包括在碱的存在下,通过化合物式i-1与x为br,Cl或f,或其盐的化合物式i-2进行反应,当x为br或cl时,在四正丁基铵氟化物水合物或氢氟酸铯的存在下进行.本发明还涉及化合物式i-1及其用途.

专利信息

专利号:WO-2025102245-A1
优先权日:2023-11-14
标题:Synthesis method for dual endothelin receptor antagonist aprocitentan
发明人：XU XIANGUANG; WANG ZHEN; ZHU GUORONG; TU YONGJUN
权利人:ZHEJIANG TIANYU PHARMACEUTICAL CO LTD
摘要:Provided in the present invention is a synthesis method for aprocitentan, comprising the following steps: 1) a compound of formula X and a sulfonylation reagent compound of formula XI undergoing a sulfonylation reaction to prepare a compound of formula XII; and 2) removing an R protective group on the pyrimidine sulfonamide compound of formula XII obtained in the previous step, so as to obtain aprocitentan. The synthesis method of the present invention overcomes the problem in the prior art that preparing macitentan by means of condensation of chloropyrimidine and sulfonamide needs to use an excessive amount of a strong base and involves a relatively low conversion efficiency, relatively many side products and other defects. The synthesis method does not need using a fluorine reagent for fluorination, involves economical steps, is environmentally-friendly, and has a relatively low comprehensive production cost. Compared with existing methods for preparing aprocitentan, the method of the present invention has characteristics of easily available raw materials, being environmentally-friendly and economical, and the like, thereby facilitating the industrial production of aprocitentan.

专利号:CN-116375652-A
优先权日:2023-03-24
标题 :A kind of directional synthesis method of process impurity R of macitentan

专利号:CN-119528820-A
优先权日:2024-11-29
标题 :Apricoxiyet Synthesis method of tam

专利号:CN-117736152-A
优先权日:2023-11-14
标题 :Synthesis method of dual endothelin receptor antagonist aprecitentan