合成目标产物 2-Thienylmagnesium Bromide Solution 主要起始原料 2-Bromothiophene And Iodomethane
(文献来源)合成步骤主要原料 2-Bromothiophene 和 Iodomethane
2-溴噻吩 反应生成 苯硫基溴化镁 参考文献: Manufacturing Process For Tiotropium Bromide[fr] Procédé De Fabrication De Bromure De Tiotropium 标题: Manufacturing Process For Tiotropium Bromide[fr] Procédé De Fabrication De Bromure De Tiotropium 摘要:本发明涉及一种用作长效抗胆碱能支气管扩张剂的药物活性化合物(i)的新型制造工艺.从公式(iii)的草酸衍生物开始,本发明描述了一种制备新型环状酐(II)的方法,该酐是在合成噻托溴铵(公式(i)化合物)过程中非常高效的前体.
专利信息
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-8680297-B2 优先权日:2011-10-06 标 题 :Manufacturing process for tiotropium bromide 发明人:SOUKUP MILAN 权利人:SOUKUP MILAN; DRUG PROCESS LICENSING ASSOC LLC 摘要:The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as a long-acting anticholinergic bronchodilator. Starting from oxalic acid derivative of formula III the invention describes preparation of a novel cyclic anhydride of formula II which is very efficient precursor in the synthesis of Tiotropium bromide (compound of formula I).
专利号:US-9024045-B2 优先权日:2012-06-04 标题 :Process for preparing styrene derivatives 发明人:GOTTA MATTHIAS; LEHNEMANN BERND WILHELM; VON WANGELIN JACOBI AXEL; GUELAK SAMET 权利人:SALTIGO GMBH 摘要:A process is provided which allows the synthesis of a large number of styrene derivatives with formation of C—C bonds, with use being possible of economically advantageous substrates, readily available carbon nucleophiles, and both inexpensive and environmentally unproblematic catalyst systems, permitting reaction under mild conditions and a high compatibility with functional groups on the reactants involved.
专利号:CN-115028641-A 优先权日:2022-07-19 标题:A method for cobalt-catalyzed synthesis of 5,8-difunctional substituted imidazo[1,2-a]pyrazine compounds
专利号:EP-2825535-B1 优先权日:2012-03-16 标 题 :A method of preparing the scopine ester of di-(2-thienyl)glycolic acid, an intermediate in the synthesis of tiotropium bromide, and its new form 发明人:CERNA IGOR; HAJICEK JOSEF 权利人:ZENTIVA KS
专利号:WO-2013135219-A1 优先权日:2012-03-16 标 题 :A method of preparing the scopine ester of di-(2-thienyl)glycolic acid, an intermediate in the synthesis of tiotropium bromide, and its new form