CAS: 154057-56-4; 3-(Bromomethyl)-2-Cyclopropyl-4-(4-Fluorophenyl)Quinoline

上下游产品

CAS号121660-11-5 2-环丙基-4-(4-氟苯基)... | CAS号6704-19-4 1-环丙基丙-1-酮 | CAS号121660-37-5 2-环丙基-4-(4-氟苯基)... | CAS号586966-54-3 匹伐他汀叔丁酯 | CAS号121660-37-5 2-环丙基-4-(4-氟苯基)... | CAS号121660-11-5 2-环丙基-4-(4-氟苯基)... | CAS号146578-99-6 匹伐他汀中间体PB3 | CAS号147489-06-3 6-[[(1E)-2-环丙基-... | CAS号147511-70-4 匹伐他汀中间体PB7

环丙基乙基甲酮置于n-溴代丁二酰亚胺(Nbs),对甲苯磺酸体系中,用 四氯化碳,甲苯,乙腈 用作溶剂,化学反应 108.0H,反应生成3-溴甲基-2-环丙基-4-(4'-氟苯基)喹啉
参考文献:Process For The Preparation Of Key Intermediates For The Synthesis Of Statins Or Pharmaceutically Acceptable Salts Thereof
标题:Process For The Preparation Of Key Intermediates For The Synthesis Of Statins Or Pharmaceutically Acceptable Salts Thereof
摘要:该发明涉及一种用于合成他汀类药物的关键中间体的商业可行过程,特别是rosuvastatin和pitavastatin,或其相应的药用盐.提供了一种新的简单和短的关键中间体合成路线,利用廉价且易获得的起始原料,避免了传统上最常用的还原剂dibal-H的使用.

专利信息

专利号:US-9085538-B2
优先权日:2010-07-26
标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof
发明人：CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO
权利人:CASAR ZDENKO; STERK DAMJAN; JUKIC MARKO; LEK PHARMACEUTICALS
摘要:The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.

专利号:US-11814355-B2
优先权日:2020-08-06
标 题 :Method for synthesizing pitavastatin t-butyl ester
发明人：HUANG HUAN; LI KAI; HUANG QINGYUN; ZHAN FUMING; HUANG QINGGUO
权利人:ANHUI QINGYUN PHARMACEUTICAL AND CHEMICAL CO LTD
摘要:A method for synthesizing pitavastatin tert-butyl ester includes obtaining a substance B through reacting (4R-CIS)-6-chloromethyl-2,2-dimethyl-1,3-dioxolane-4-acetic acid tert-butyl ester with a substance A under the action of a first base catalyst, 5 oxidizing with an oxidizing agent to obtain a substance C, then reacting with 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-formaldehyde under the action of a second base catalyst to obtain a substance D, and finally, carrying out an acid deprotection to obtain pitavastatin t-butyl ester. The reaction conditions of the present invention are mild and controllable, and the reaction conditions of the synthesis of the Julia olefination do 10 not require an ultra-low temperature reaction. The operation is convenient and simple, the stereoselectivity is good, the yield is high, and the synthesized pitavastatin t-butyl ester is a completely non-cis isomer, and its purity is high.

专利号:US-2014051854-A1
优先权日:2010-07-26
标题 :Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof

专利号:WO-2012013325-A1
优先权日:2010-07-26
标题 :Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof

专利号:EP-2423195-A1
优先权日:2010-07-26
标题 :Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof

专利号:EP-2598484-B1
优先权日:2010-07-26
标题:Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof