CAS: 866030-35-5; Tert-Butyl ((1S,3S)-1-((2S,4S)-4-Isopropyl-5-Oxotetrahydrofuran-2-yl)-3-(4-Methoxy-3-(3-Methoxypropoxy)Benzyl)-4-Methylpentyl)Carbamate

上下游产品

CAS号24424-99-5 二碳酸二叔丁酯 | CAS号173336-76-0 4-溴-1-甲氧基-2-(3-... | CAS号866030-34-4 ((1S,2S,4S)-2-h... | CAS号324763-46-4 5(S)-[1(S)-叠氮基-... | CAS号934841-22-2 N-[(1S,3S)-3-[4... | CAS号1310055-52-7 (3S,5S)-3-isopr... | CAS号878276-64-3 (2S,5S,7S)-5-te... | CAS号173334-57-1 阿利吉仑 | CAS号173338-07-3 [1S-[1R*(R*),2R...

[(1S,3S)-3-[[4-甲氧基-3-(3-甲氧基丙氧基)苯基]甲基]-4-甲基-1-[(2S)-四氢-5-氧代-2-呋喃基]戊基]氨基甲酸苄酯置于五氯化磷,三乙胺,Lithium Hexamethyldisilazane体系中,用 四氢呋喃,正己烷,二氯甲烷 作为反应溶剂,化学反应 72.5H,反应生成 [(1S,3S)-3-[[4-甲氧基-3-(3-甲氧基丙氧基)苯基]甲基]-4-甲基-1-[(2S,4S)-四氢-4-异丙基-5-氧代-2-呋喃基]戊基]-氨基甲酸叔丁酯
参考文献:强大的肾素抑制剂阿利吉仑的正式全合成:Smi 2促进的酰基样自由基偶联剂的应用
标题:强大的肾素抑制剂阿利吉仑的正式全合成:Smi 2促进的酰基样自由基偶联剂的应用
摘要:公开了有效的肾素抑制剂阿利吉仑的正式全合成,其利用了由该实验室最近开发的用于制备基于羟乙烯等排酯的一类蛋白酶抑制剂的替代偶联策略.通过smi硫酯衍生物表示阿利吉仑碳骨架的c5-C9片段的氨基酸的进行了碳链延长2促进的自由基加成到ñ丙烯酸丁酯.具有正确的相对构型的c 3-异丙基的引入是通过伴随内酯化的立体选择性还原获得的酮,然后与丙酮进行醛醇缩合反应而完成的.进一步的官能团和保护基团的操作最终使阿利吉仑从相应的受完全保护的非天然氨基酸开始进行正式的全合成,最终完成了10个步骤.
DOI:10.1021/jo060296C

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-7973175-B2
优先权日:2005-09-28
标 题 :Synthesis of renin inhibitors involving a cycloaddition reaction
发明人：MICKEL STUART J; MARTERER WOLFGANG
权利人: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 III, n nwherein R, R 1 , and R′ are as defined in the specification, or a salt thereof, and a compound of formula IVn n nwherein R, R 1 , R 2 and R′ are as defined in the specification, and processes of manufacturing these.

专利号:US-9056816-B2
优先权日:2011-10-25
标 题:Process for the preparation of aliskiren
发明人：BISWAS SUJAY; SRIMURUGAN SANKARESWARAN; KUMAR ANJUL; PANDA ATULYA KUMAR; JAMSHAD DANISH; MASAND MUKESH; BISWAS BIDYUT; BANSAL VIKAS; GUPTA ASHISH KUMAR; VIR DHARAM
权利人:JUBILANT LIFE SCIENCES LTD
摘要:The present invention provides a novel process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, or a salt thereof, preferably Aliskiren hemifumarate.

专利号:WO-2011127797-A1
优先权日:2010-04-12
标 题:Intermediates for synthesis of aliskiren and their preparation
发明人：ZHANG FUYAO; SUN PIAOYANG
权利人:UNITRIS BIOPHARMA CO LTD; ZHANG FUYAO; SUN PIAOYANG
摘要:Aliskiren intermediates and their preparation methods are provided. Specifically aliskiren intermediates present by formula (I), formula (II) and formula (III) and their preparation methods are provided. The nitro-aldol reaction of the intermediates of formula (II) and formula (III) can provide the intermediates of formula (I) which can subsequently be converted to 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-8338620-B2
优先权日:2007-04-03
标 题:Methods for the production of C-8 lactam lactone compounds
发明人：SEDELMEIER GOTTFRIED
权利人:SEDELMEIER GOTTFRIED; 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, the invention relates to a process for the manufacture of a compound of the formula I, n nor a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.