CAS: 160970-54-7; 1-(3-Hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2-Trifluoroethoxy)Phenoxy]Ethylamino]Propyl]-2,3-Dihydroindole-7-Carboxamide

上下游产品

1-(3-hydroxypropyl)-5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl]-2,3-dihydro-1H-indole-7-carbonitrile 2-methoxy-phenol benzene-1,2-diol 5-[(2R)-2-aminopropyl]-2,3-dihydro-1-[3-(benzoyloxy)propyl]-1H-indole-7-carbonitrile(R)-tert-butyl 1-(7-carbamoyl-1-(3-hydroxypropyl)indolin-5-yl)propan-2-yl(2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)carbamate

3-(7-Cyano-5-[(2R)-2-(2-[2-(2,2,2-Trifluoroethoxy)Phenoxy]Ethylamino)Propyl]-2,3-Dihydro-1H-Indol-1-yl)Propylbenzoate (2R,3R)-Tartrate Salt置于水,Sodium Hydroxide,双氧水体系中,用 甲醇,水,二甲基亚砜 用作溶剂,化学反应 24.0H,以43%的收率获得西洛多辛
参考文献:1−(3−ベンゾイルオキシプロピル)−7−シアノ−5−[(2r)−2−({2−[2−(2,2,2−トリフルオロエトキシ)フェノキシ]エチル}アミノ)プロピル]インドリンまたはその塩を製造する方法
标题:1−(3−ベンゾイルオキシプロピル)−7−シアノ−5−[(2r)−2−({2−[2−(2,2,2−トリフルオロエトキシ)フェノキシ]エチル}アミノ)プロピル]インドリンまたはその塩を製造する方法
摘要:提供一种高纯度的1-(3-苯甲酰氧丙基)-7-氰-5-[(2R)-2-({2-[2-(2,2,2-三氟乙氧基)苯氧基]乙基}氨基)丙基]吲哚的高效制备方法,其中特定杂质量减少.使用低极性有机溶剂和水的混合物作为反应溶剂,进行5-(2-氨基丙基)-1-(3-苯甲酰氧丙基)-7-氰吲哚中氨基的亲核取代反应.[选择图]无

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:WO-2011101864-A1
优先权日:2010-02-17
标题 :Novel process for the synthesis of phenoxyethyl derivatives
发明人：JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA
权利人:PANACEA BIOTEC LTD; JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA
摘要:The present invention provides an improved process for the synthesis of 2-[2- (2,2,2-trifluoroethoxy)phenoxy]ethanol intermediate, its derivatives and/or its pharmaceutically acceptable salts, useful in the synthesis of α-1 adrenoceptor blockers such as silodosin.

专利号:WO-2012131710-A3
优先权日:2011-03-30
标题:Novel process for the synthesis of indoline derivatives
发明人：JAIN RAJESH; RAO JAGADEESHWAR R; RAO SIRIPRAGADA MAHENDER
权利人:PANACEA BIOTEC LTD; JAIN RAJESH; RAO JAGADEESHWAR R; RAO SIRIPRAGADA MAHENDER
摘要:The present invention provides a process for the synthesis of indoline intermidiate useful in the synthesis of α-1 adrenoceptor blockers such as silodosin. Indoline intermediate has following formula: (where R is hydroxy or protecting group) and is preferably a tartrate salt.

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-2015158809-A9
优先权日:2013-02-26
标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
权利人:XENOPORT INC
摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

专利号:US-2005187222-A1
优先权日:1996-02-02
标题:Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds
发明人：GARVEY DAVID S; DE TEJADA INIGO S; GASTON RICKY D; KHANAPURE SUBHASH P; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.