CAS: 173336-76-0; 4-Bromo-1-Methoxy-2-(3-Methoxypropoxy)Benzene

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CAS号36215-07-3 1-氯-3-甲氧基丙烷 | CAS号37942-01-1 5-溴-2-甲氧基苯酚 | CAS号36865-41-5 1-溴-3-甲氧基丙烷 | CAS号173334-57-1 阿利吉仑 | CAS号1236549-06-6 δN-苄氧基羰基阿利克仑 | CAS号173338-07-3 [1S-[1R*(R*),2R... | CAS号866030-35-5 [(1S,3S)-3-[[4-... | CAS号919995-27-0 1-(4-甲氧基-3-(3-甲... | CAS号934841-22-2 N-[(1S,3S)-3-[4...

3-氯丙基甲基醚,5-溴-2-甲氧基苯酚置于potassium Carbonate,Sodium Iodide体系中,用 乙腈 用作溶剂,以95%的收率获得4-溴-1-甲氧基-2-(3-甲氧基丙氧基)苯
参考文献:全合成" Aliskiren":高血压临床实践中的第一种肾素抑制剂
标题:全合成" Aliskiren":高血压临床实践中的第一种肾素抑制剂
摘要:我们报告了从目前的"异丙基卡隆"开始使用高度立体控制的方法,向阿利吉仑("阿利吉仑")迈进的"宏观周期路线",阿利吉仑目前是一种用于治疗高血压的药物.合成的重点包括具有挑战性的rcm反应,该反应可产生九元不饱和内酯,高度立体选择性的催化du Bois叠氮化和对邻氨基氨基醇的区域和非对映选择性氮丙啶开环.
Doi:10.1021/ol100427V

专利信息

专利号:US-8198465-B2
优先权日:2005-10-17
标 题 :3-alkyl-5- (4-alkyl-5-oxo-tetrahydrofutran-2-yl) pyrrolidin-2-one derivatives as intermediates in the synthesis of renin inhibitors
发明人：SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT
权利人:SEDELMEIER GOTTFRIED; GRIMLER DOMINIQUE; ACEMOGLU MURAT; NOVARTIS AG
摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula II, n nor a salt thereof, and a compound of formula VIn n nor a salt thereof, wherein R 3 and R 4 as well as Act are as defined in the specification, and processes of manufacturing these.n n Additionally transformation of compounds (VI) with metallo organic compounds (VII) give rise to the new compounds (VIII) which are direct precursors for the preparation of Aliskiren.

专利号:US-8143416-B2
优先权日:2004-08-31
标题 :Alternative synthesis of renin inhibitors and intermediates thereof
发明人：SEDELMEIER GOTTFRIED; MICKEL STUART JOHN; RUEEGER HEINRICH
权利人:SEDELMEIER GOTTFRIED; MICKEL STUART JOHN; RUEEGER HEINRICH; NOVARTIS AG
摘要:The present invention relates to synthetic routes to prepare a compound of the formula n nwherein R 1 is halogen, C 1-6 halogenalkyl, C 1-6 alkoxy-C 1-6 alkyloxy or C 1-6 alkoxy-C 1-6 alkyl; R 2 is halogen, C 1-4 alkyl or C 1-4 alkoxy; R 3 and R 4 are independently branched C 3-6 alkyl; and R 5 is cycloalkyl, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy-C 1-6 alkyl, C 1-6 alkanoyloxy-C 1-6 alkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, C 1-6 dialkylamino-C 1-6 alkyl, C 1-6 alkanoylamino-C 1-6 alkyl, HO(O)C—C 1-6 alkyl, C 1-6 alkyl-O—(O)C—C 1-6 alkyl, H 2 N—C(O)—C 1-6 alkyl, C 1-6 alkyl-HN—C(O)—C 1-6 alkyl or (C 1-6 alkyl) 2 N—C(O)—C 1-6 alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.

专利号:US-2008262246-A1
优先权日:2005-10-17
标 题:3-Alkyl-5- (4-Alkyl-5-Oxo-Tetrahydrofutr An -2-Yl) Pyrrolidin-2-One Derivatives As Intermediates In The Synthesis Of Renin Inhibitors

专利号:US-2007208055-A1
优先权日:2004-08-31
标题 :Alternative synthesis of renin inhibitors and intermediates thereof

专利号:US-7910774-B2
优先权日:2004-08-31
标题:Alternative synthesis of renin inhibitors and intermediates thereof

专利号:WO-2006024501-A1
优先权日:2004-08-31
标 题 :Alternative synthesis of renin inhibitors and intermediates thereof