CAS: 172900-75-3; 4-Methoxy-3-(3-Methoxypropoxy)Benzaldehyde

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CAS号621-59-0 异香兰素； 3-羟基-4-甲氧... | CAS号36865-41-5 1-溴-3-甲氧基丙烷 | CAS号1589-49-7 3-甲氧基-1-丙醇 | CAS号67-56-1 甲醇 | CAS号148433-01-6 3-(3-bromopropo... | CAS号324763-39-5 阿利克仑-1 | CAS号324763-46-4 5(S)-[1(S)-叠氮基-... | CAS号387353-71-1 (2S,4E,7R)-7-[4... | CAS号173334-57-1 阿利吉仑 | CAS号866030-33-3 (2S,5R)-3,6-二乙氧... | CAS号866030-36-6 [(1S,3S)-3-[4-甲... | CAS号324763-47-5 (αS,γS,δS,ζS)-N... | CAS号172900-73-1 4-(溴甲基)-1-甲氧基-2... | CAS号172900-74-2 3-(3-甲氧基丙氧基)-4-... | CAS号172900-69-5 (R)-[2-溴甲基-3-甲基...

📜异香兰素置于sodium Methylate,Potassium Carbonate体系中,用 甲醇,乙腈 用作溶剂,化学反应 20.5H,反应生成3-(3-甲氧基丙氧基)-4-甲氧基苯甲醛
参考文献:非手性双laclactim二乙氧基醚作为立体定向合成γ-支链的α-氨基酸的立体诱导合成子:一种实用的大规模途径,以新型的肾素抑制剂阿利吉仑的中间体.
标题:非手性双laclactim二乙氧基醚作为立体定向合成γ-支链的α-氨基酸的立体诱导合成子:一种实用的大规模途径,以新型的肾素抑制剂阿利吉仑的中间体.
摘要:位阻γ-支链α-氨基酸衍生物(2 S,4 S)-24A及其受n-[(叔丁氧基)羰基](boc)保护的醇(2 S,4 S)的非对映选择性合成-19,一类新的非肽肾素抑制剂,例如阿利吉仑(均为关键中间体1中所述).最初,类似的甲基酯(2小号,4小号)-17由手性烷基化得到schöllkopf二氢吡嗪([r )-12A与二烷氧基取代的烷基溴([r )-11A,其与显式高diastereofacial选择性(进行ds >=98%),得到(2小号,5-[r,2'小号)-13A(方案4),其次是温和的酸水解和n-Boc保护(方案5).相反,建议除了(i)预期的屏蔽作用外,对于(R)-11A与对映异构体(S)-12B的反应,完全缺乏立体控制且收率很低.所述meoc(6)和的大残基(间的辅助,空间排斥的pr基的c(2)-[r )-11A在所提出的过渡状态,这将强烈不利于两者的si和
Doi:10.1002/hlca.200390235

专利信息

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:WO-2011148392-A1
优先权日:2010-05-28
标题 :Process for the preparation of (2s,4s,5s,7s)-n-(2-carbamyl-2- methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3- methoxypropoxy)phenyl]-octanamide hemifumarate and its intermediates thereof
发明人：SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY
权利人:MSN LAB LTD; SATYANARAYANA REDDY MANNE; THIRUMALAI RAJAN SRINIVASAN; ESWARAIAH SAJJA; VENKAT REDDY GHOJALA; RAMA SUBBA REDDY KARAMALA; SAHADEVA REDDY MARAMREDDY
摘要:The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.

专利号:EP-1836163-B1
优先权日:2004-12-23
标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin
发明人：BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER
权利人:NOVARTIS AG
摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

专利号:ES-2358536-T3
优先权日:2005-09-28
标题 :SYNTHESIS OF RENINAL INHIBITORS INVOLVING A CYCLOADITION REACTION.

专利号:US-2008255369-A1
优先权日:2005-09-28
标 题 :Synthesis of Renin Inhibitors Involving a Cycloaddition Reaction

专利号:US-9346745-B2
优先权日:2010-06-04
标题:Process for producing Aliskiren
发明人：TADDEI MAURIZIO; RUSSO ADELE; CINI ELENA; RIVA RENATA; RASPARINI MARCELLO; CARCONE LUCA; BANFI LUCA; VITALE ROMINA; ROSEBLADE STEPHEN; ZANOTTI-GEROSA ANTONIO CARLO
权利人:TADDEI MAURIZIO; RUSSO ADELE; CINI ELENA; RIVA RENATA; RASPARINI MARCELLO; CARCONE LUCA; BANFI LUCA; VITALE ROMINA; ROSEBLADE STEPHEN; ZANOTTI-GEROSA ANTONIO CARLO; CHEMO IBERICA SA
摘要:A new route of synthesis of the compound Aliskiren of formula (I), used in the treatment of hypertension, is described.