CAS: 173334-57-1; (2S,4S,5S,7S)-5-Amino-N-(3-Amino-2,2-Dimethyl-3-Oxopropyl)-4-Hydroxy-2-Isopropyl-7-(4-Methoxy-3-(3-Methoxypropoxy)Benzyl)-8-Methylnonanamide

上下游产品

(2S,4S,5S,7S)-N-(3-amino-2,2-dimethyl-3-oxopropyl)-5-azido-4-hydroxy-2-isopropyl-7-(4-methoxy-3-(methoxypropoxy)benzyl)-8-methylnonanamide tert-butyl (3S,5S,6S,8S)-8-(3-amino-2,2-dimethyl-3-oxopropylcarbamoyl)-6-hydroxy-3-(4-methoxy-3-(3-methoxypropoxy)benzyl)-2,9-dimethyldecan-5-ylcarbamate (2-carbamoyl-2-methylpropyl)carbamic acid benzyl ester (1S,3S)-{1-formyl-3-[4-methoxy-3-(3-methoxy-propoxy)-benzyl]-4-methyl-pentyl}-carbamic acid tert-butyl ester 2(S),4(S),5(S),7(S)-N-(3-amino-2,2-dimethyl-3-oxopropyl)-2,7-di(1-methylethyl)-4-hydroxy-5-amino-8-[4-methoxy-3-(3-methoxypropoxy)phenyl]°Ctanamide nitrate (2S,4S,5S,7S)-5-amino-N-(3-amino-2,2-dimethyl-3-oxypropyl)-4-hydroxy-7-[[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl]-8-methyl-(2-propan-2-yl)nonanamide hemifumarate (2S),(4S),(5S),(7S)-N-(3-amino-2,2-dimethyl-3-oxopropyl)-2,7-di(1-methylethyl)-4-hydroxy-5-amino-8-[4-methoxy-3-(3-methoxy-propoxy)phenyl]-°Ctanamide L-malate aliskiren glycolic acid salt

甘露醇置于palladium 10% On Activated Carbon 吡啶,2-羟基吡啶,盐酸,Sodium Periodate,正丁基锂,Sodium Azide,(2-氨基-1,1-二甲基乙基)二甲基胺,氢气,四丁基硫酸氢铵,碳酸氢钠,对甲苯磺酸,三乙胺,三苯基膦,三氟乙酸,Lithium Hexamethyldisilazane,偶氮二甲酸二乙酯,三氯氧磷,对硝基苯甲酸体系中,用 四氢呋喃,四氢吡喃,甲醇,二氯甲烷,水,N,N-二甲基甲酰胺,丙酮,乙腈 用作溶剂,-78.0~90.0 °C,413.7 Kpa 条件下,反应 159.16H,反应生成阿利克仑
参考文献: A Novel Process For Making Aliskiren,Its Novel Intermediates And Certain Novel Compounds[fr] Nouveau Procédé De Production D'Aliskirène,Ses Nouveaux Intermédiaires Et Certains Nouveaux Composés
标题: A Novel Process For Making Aliskiren,Its Novel Intermediates And Certain Novel Compounds[fr] Nouveau Procédé De Production D'Aliskirène,Ses Nouveaux Intermédiaires Et Certains Nouveaux Composés
摘要:揭示了一种制备类似阿利斯基仑的肾素抑制剂的新型工艺.同时还披露了其新型中间体化合物和制备方法.

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

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-2012149895-A1
优先权日:2009-04-01
标题 :Process for dimethylation of active methylene groups
发明人：JENKO BRANKO; COPAR ANTON
权利人:JENKO BRANKO; COPAR ANTON; LEK PHARMACEUTICALS
摘要:The present invention discloses a process for dimethylation of active methylene groups. Specifically, the invention discloses a process for preparing 3-amino-2,2-dimethylpropanamide. Compounds produced by the present dimethylation process such as 3-amino-2,2-dimethylpropanamide can be used as intermediates in the route of synthesis of therapeutic, prophylactic or diagnostic agent, for example aliskiren or cryptophycin. Particularly, the invention relates to embodiments further extending to processes for preparing pharmaceutical dosage form comprising said therapeutic, prophylactic or diagnostic agents. More specifically, the invention relates to the use of compounds produced by the present dimethylation process for the manufacture of therapeutic, prophylactic or diagnostic agents or for the manufacture of pharmaceutical dosage forms comprising said therapeutic, prophylactic or diagnostic agents. The processes according to the present invention can be beneficially applied for the synthesis of various active pharmaceutical ingredients, such as aliskiren or crypthophycin.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

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.