CAS: 289042-11-1; Methyl 4-(4-Fluorophenyl)-6-Isopropyl-2-(N-Methylmethylsulfonamido)Pyrimidine-5-Carboxylate

相似化合物

147118-37-4 147118-36-3 1263475-93-9

上下游产品

CAS号799842-06-1 4-(4-氟苯基)-6-异丙基... | CAS号41881-75-8 sodium salt of ... | CAS号160009-36-9 4-(4-氟苯基)-2-(甲基... | CAS号124-63-0 甲基磺酰氯 | CAS号1184-85-6 N-甲基甲磺酰胺 | CAS号160009-37-0 2-氨基-4-(4-氟苯基)-... | CAS号14593-46-5 叔戊醇钠 | CAS号289042-10-0 瑞舒伐他汀中间体Z-8.1 | CAS号147118-36-3 4-(4-氟苯基)-6-异丙基...

瑞舒伐他汀钙中间体rsb-3置于sodium Hydride,N,N-二甲基苯胺,三氯氧磷体系中,用 乙腈,Mineral Oil 用作溶剂,化学反应 9.58H,反应生成4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-羧酸甲酯
参考文献:瑞舒伐他汀钙核的高效构建
标题:瑞舒伐他汀钙核的高效构建
摘要:建立了瑞舒伐他汀核心的新颖高效的五步合成路线,包括biginelli反应,脱氢,氯化,磺酰胺化和还原.系统地研究了所有步骤.将叔丁基过氧化氢水溶液代替硝酸用于脱氢.以n,N-二甲基苯胺为催化剂,促进氯化反应的顺利进行,并探讨了其催化机理.在磺酰胺化中,使用nah和乙腈可明显提高化合物5的转化率.此外,还有两个磺酰胺化副产物6和7被检测并隔离.因此,在优化的反应条件下,以60.4%的总收率获得目标产物,远高于报道的收率(36.4%).
Doi:10.1002/jhet.2785

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: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

专利号:WO-2007074391-A2
优先权日:2005-12-28
标题:Preparation of a key intermediate in the synthesis of rosuvastatin