CAS: 147118-36-3; 4-(4-Fluorophenyl)-6-Isopropyl-2-[(N-Methyl-N-Methylsufonyl)Amino]Pyrimidine-5-Yl-Methanol

上下游产品

CAS号147118-30-7 4-(4-氟苯基)-6-异丙基... | CAS号1263475-93-9 4-(4-氟苯基)-6-异丙基... | CAS号799842-07-2 瑞舒伐他中间体Z-8 | CAS号289042-11-1 瑞舒伐他汀中间体Z-6 | CAS号953776-62-0 N-[4-(4-fluorop... | CAS号147118-37-4 4-(4-氟苯基)-6-异丙基... | CAS号114433-94-2 1-(4-氟苯基)-4-甲基-... | CAS号1207460-34-1 4-(4-fluorophen... | CAS号459-57-4 对氟苯甲醛 | CAS号503610-43-3 瑞舒伐他汀-5S-内酯 | CAS号289042-12-2 6-[(1E)-2-[4-(4... | CAS号799842-07-2 瑞舒伐他中间体Z-8 | CAS号289042-10-0 瑞舒伐他汀中间体Z-8.1 | CAS号147118-40-9 瑞舒伐他汀中间体H-3 | CAS号147118-39-6 瑞舒伐他汀中间体H-2 | CAS号147118-37-4 4-(4-氟苯基)-6-异丙基... | CAS号147118-38-5 7-[4-(4-氟苯基)-6-... | CAS号1221497-92-2 P-[[4-(4-Fluoro...

1-(4-氟苯基)-4-甲基戊-1,3-二酮置于n-溴代丁二酰亚胺(Nbs),Potassium Tert-Butylate,水,Potassium Carbonate,三乙胺体系中,用 四氢呋喃,二氯甲烷,丙酮,乙腈,叔丁醇 用作溶剂,化学反应 102.0H,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-甲醇
参考文献:鲁苏伐他汀合成中三种关键嘧啶前体的简便高效方法
标题:鲁苏伐他汀合成中三种关键嘧啶前体的简便高效方法
摘要:我们报道了5-甲酰基-,5-(羟甲基)-和5-(溴甲基)取代的n-[4-(4-氟苯基)-6-异丙基嘧啶-2-基]-N-甲基甲磺酰胺的合成.提出的合成方法基于高效的三步制备功能化的5-甲基嘧啶.通过nbs在辐射下将甲基选择性地溴化成溴甲基衍生物,然后将其以接近定量的收率转化为羟甲基或甲酰基.该方法优于现有的制备用于合成瑞舒伐他汀的关键嘧啶前体的方法,因为它不涉及金属催化和低温反应条件.
Doi:10.1016/j.Tet.2012.01.013

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-9376397-B2
优先权日:2009-02-02
标 题 :Key intermediates for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof
发明人：CASAR ZDENKO; KOSMRLJ JANEZ
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates in general to the field of organic chemistry and in particular to the preparation of N-(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)-N-methylmethanesulfonamide (I), N-(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (II) and N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.

专利号:US-8354530-B2
优先权日:2005-07-28
标 题:Process for the synthesis of rosuvastatin calcium
发明人：ZLICAR MARKO
权利人:LEK PHARMACEUTICALS; ZLICAR MARKO
摘要:Present invention represents process for the preparation of HMG-CoA reductase inhibitors, in particular rosuvastatin calcium introducing L-malic acid as the source of chirality for the side chain.

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:US-2008255170-A1
优先权日:2005-07-28
标题 :Process for the Synthesis of Rosuvastatin Calcium

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