CAS: 289042-10-0; N-(5-((Diphenylphosphoryl)Methyl)-4-(4-Fluorophenyl)-6-Isopropylpyrimidin-2-yl)-N-Methylmethanesulfonamide

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4-(4-氟苯基)-6-异丙基-2-[(N-甲基-N-甲磺酰)氨基]嘧啶-5-甲醇置于三溴化磷体系中,用 甲苯,乙腈 用作溶剂,化学反应 1.0H,反应生成N-[5-(联苯-膦酰基甲基)-4-(4-氟-苯基)-6-异丙基-嘧啶-2-基]-N-甲基-甲烷磺胺
参考文献:原位形成的烯丙基半缩醛的钯催化立体选择性环化:瑞舒伐他汀和匹伐他汀的合成
标题:原位形成的烯丙基半缩醛的钯催化立体选择性环化:瑞舒伐他汀和匹伐他汀的合成
摘要:描述了非对映选择性钯催化的烯丙基半缩醛的环化.它允许选择性合成1,3-二恶烷衍生物,这是在所有他汀类药物代表中出现的顺式1,3-二醇的前体.该反应允许以简单的方式完全合成瑞舒伐他汀和匹伐他汀.
Doi:10.1021/acs.Orglett.8B01156

专利信息

专利号:US-6160115-A
优先权日:1999-03-10
标 题:Process for preparing N-[5-(diphenylphosphinoylmethyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin -2-yl]-N-methylmethanesulfonamide
发明人：BRIEDEN WALTER; VEITH ULRICH
权利人:LONZA AG
摘要:N-[5-(Diphenylphosphinoylmethyl)-4-(4-fluorophenyl)-6-isopropylpyrimid in-2-yl]-N-methylmethanesulfonamide of the formula: is prepared by reaction of [4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyri midin-5-yl]methanol with chlorodiphenylphosphine. Compound I is an intermediate in the synthesis of pharmaceutically active compounds, in particular HMG-Co A. reductase inhibitors.