CAS: 256431-72-8; (E)-3-(2-Cyclopropyl-4-(4-Fluorophenyl)Quinolin-3-yl)Acrylonitrile

相似化合物

121660-37-5 154057-56-4 148901-68-2

上下游产品

CAS号121660-43-3 2-cyclopropyl-4... | CAS号121660-18-2 (2-cyclopropyl-... | CAS号121660-11-5 2-环丙基-4-(4-氟苯基)... | CAS号2537-48-6 氰甲基磷酸二乙酯 | CAS号121660-37-5 2-环丙基-4-(4-氟苯基)... | CAS号147526-32-7 匹伐他汀钙 | CAS号148901-69-3 (E)-7-[2-环丙基-4-... | CAS号148901-68-2 (E)-3-[2-环丙基-4-... | CAS号254452-86-3 (3S,5R,6E)-7-[2...

[2-Cyclopropyl-4-(4-Fluoro-Phenyl)-6,7-Dimethoxy-Quinolin-3-Yl]-Methanol置于sodium Hydroxide,正丁基锂,Sodium Acetate,甲基三辛基氯化铵,Pyridinium Chlorochromate体系中,用 四氢呋喃,正己烷,二氯甲烷,甲苯 用作溶剂,化学反应 2.0H,反应生成(E)-3-[2-环丙基-4-(4-氟苯基)-3-喹啉基]-2-丙烯腈
参考文献:喹啉基hmg-Coa还原酶抑制剂的合成和生物学评估.
标题:喹啉基hmg-Coa还原酶抑制剂的合成和生物学评估.
摘要:由喹啉羧酸酯经同源,醛基与乙酰乙酸乙酯双阴离子缩醛反应和3-羟基酮还原合成了一系列基于喹啉的3,5-二羟基庚酸衍生物,以评价其体外抑制hmg-Coa还原酶的能力.与先前的文献一致,在外环上存在严格的结构要求,并且4-氟苯基在该系统中最活跃.对于中心环,在中心喹啉核的6,7和8位上的取代会适度影响效价,而在2位上的烷基侧链对活性有更明显的影响.在衍生物中,具有环丙基作为烷基侧链的nk-104(匹伐他汀钙)显示出最大的效力.
Doi:10.1016/s0968-0896(01)00198-5

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-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-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