环丙基乙基甲酮置于sodium Iodide N-溴代丁二酰亚胺(Nbs),水,碳酸氢钠,对甲苯磺酸,二甲基亚砜体系中,用 四氢呋喃,四氯化碳,甲苯,乙腈 用作溶剂,化学反应 232.0H,反应生成2-环丙基-4-(4-氟苯基)喹啉-3-甲醛 参考文献: Process For The Preparation Of Key Intermediates For The Synthesis Of Statins Or Pharmaceutically Acceptable Salts Thereof[fr] Procédé De Préparation D'Intermédiaires Clés Pour La Synthèse De Statines Ou Sels Pharmaceutiquement Acceptables De Ceux-Ci 标题: Process For The Preparation Of Key Intermediates For The Synthesis Of Statins Or Pharmaceutically Acceptable Salts Thereof[fr] Procédé De Préparation D'Intermédiaires Clés Pour La Synthèse De Statines Ou Sels Pharmaceutiquement Acceptables De Ceux-Ci 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工艺,特别是用于制备罗伪司汀和匹伐司汀或其相应的药用盐.提出了一种新的简单和短路的关键中间体合成路线,其受益于使用廉价且易获得的起始原料,从而避免了传统上最常用的dibal-H还原剂.
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-9932361-B2 优先权日:2013-02-20 标题:Convenient process for the preparation of statins 发明人:DE LUCCHI OTTORINO; TARTAGGIA STEFANO; FERRARI CLARK; GALVAGNI MARCO; PONTINI MARTA; FOGAL STEFANO; MOTTERLE RICCARDO; MORENO ROSA MARIA; COMELY ALEX 权利人:F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.
专利号:US-8987478-B2 优先权日:2011-12-09 标 题:Process for the preparation of a statin precursor 发明人:DE LANGE BEN; HEEMSKERK DENNIS; BESSEMBINDER KARIN HENDERIKA MARIA 权利人:DSM SINOCHEM PHARM NL BV 摘要:The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.
专利号:US-9260423-B2 优先权日:2011-12-09 标 题:Process for the preparation of a thioprecursor for statins 发明人:DE LANGE BEN; HEEMSKERK DENNIS; BESSEMBINDER KARIN HENDERIKA MARIA 权利人:DSM SINOCHEM PHARM NL BV 摘要:The present invention relates to a process for the preparation of a precursor for the synthesis of hexanoic acid derived statins and to the use of said precursor in the manufacture of a medicament.
专利号:US-7193086-B2 优先权日:2001-05-30 标题:Process for preparation of a quinolinecarbaldehyde 发明人:MATSUMOTO HIROO; SHIMIZU TAKANORI 权利人:DAICEL CHEM 摘要:A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde important as intermediate for the synthesis of pharmaceuticals, efficiently from an unnecessary antipode, is provided. n A process for producing 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-carbaldehyde represented by the formula (III): n nwhich comprises treating a compound represented by the formula (I) or (II):n n n(wherein A is —CHOH or —C(O)—, and R is a hydrogen atom, a C 1-4 alkyl group which may be branched, a phenyl group, an alkali metal ion or an alkaline earth metal ion) with ozone, followed by reduction with an inorganic sulfur compound or by hydrogenation for reduction decomposition.
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.
参考标题:Synthesis Of Spirooxindole Analogues From 2-Cyclopropyl-4-(4-Fluorophenyl)Quinoline-3-Carbaldehyde 作者:Venkata Nookaapparao Gorli,Rajagopal Srinivasan |发布日期:2020.2.16 摘要:Abstract A Series Of Spirooxindoles Have Been Synthesized Through 1,3-Dipolar Cycloaddition Of An Azomethine Ylide Generated From Isatin And Sarcosine Or L-Proline With The Dipolarophile (E)-3-(2-Cyclopropyl-5-(4-Fluorophenyl) Quinolin-3-Yl)-1-Phenylprop-2-En-1-One Derivatives. The Stereochemistry Of The Cycloadducts Was Assigned Based On The Single-Crystal X-Ray. Graphical Abstract