CAS: 144494-65-5; (S)-2-(Butylsulfonamido)-3-(4-(4-(Piperidin-4-yl)Butoxy)Phenyl)Propanoic Acid

上下游产品

CAS号149490-61-9 N-丁磺酰基-(4-(4-吡啶... | CAS号108-89-4 4-甲基吡啶

📜4-甲基吡啶置于palladium On Activated Charcoal 盐酸,氢氧化钾,正丁基锂,氢气,Potassium Iodide体系中,用 溶剂黄146,二甲基亚砜 用作溶剂,-65.0~65.0 °C,275.79 Kpa 条件下,反应 44.5H,反应生成替罗非班
参考文献:纤维蛋白原受体拮抗剂mk-383的实用合成.(S)-酪氨酸的选择性功能化
标题:纤维蛋白原受体拮抗剂mk-383的实用合成.(S)-酪氨酸的选择性功能化
摘要:实用的四步合成纤维蛋白原受体拮抗剂mk-383,N-(正丁烷磺酰基)-O-(4-(4-哌啶基)-丁基)-(S)-酪氨酸,其总收率为48% (S)-酪氨酸.重点包括:(1)双重使用4-甲基吡啶作为哌啶的掩蔽形式,并用作与3-溴-1-氯丙烷进行3碳同源的亲核试剂前体;(2)使用三甲基甲硅烷基基团暂时保护(S)-酪氨酸的酚和羧酸氧,从而可以高产率地进行选择性的n-磺酰化;(3)使用koh / Dmso水溶液,在不消旋的情况下,高产率地对酪氨酸衍生物进行选择性的酚o-烷基化;(4)在酪氨酸环存在下,在乙酸中使用pd / C对吡啶环进行选择性加氢.
Doi:10.1016/s0040-4020(01)87943-6

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-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-2025223262-A1
优先权日:2022-03-31
标 题 :Synthesis of morphinans with reduced herg activity and mop binding
发明人：LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA
权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG
摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.

专利号:US-8183409-B2
优先权日:2004-05-06
标题:High yield and rapid synthesis methods for producing metallo-organic salts
发明人：CHRISTGAU STEPHAN; ANDERSEN JENS E T
权利人:CHRISTGAU STEPHAN; ANDERSEN JENS E T; OSTEOLOGIX AS
摘要:A new method for preparing salts of metal cations and organic acids, especially divalent salts of alkaline earth metal ions from group II of the periodic system and carboxylic acids. The method comprising the use of a high temperature (about 90° or more) and, optionally. high pressure, in order to obtain a higher yield, purity and faster reaction speed than obtained with known synthesis methods. In particular, the present invention relates to the production of strontium salts of carboxylic acids. Novel strontium salts are also provided by the present method.

专利号:US-2007287734-A1
优先权日:2006-06-09
标 题 :Preparation and utility of substituted pyrazole compounds with cannabinoid receptor activity
发明人：GANT THOMAS G; SARSHAR SEPEHR
权利人:AUSPEX PHARMACEUTICALS INC
摘要:The present disclosure is directed to modulators of CB-1 type receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of the severity and duration of obesity, metabolic syndrome, dyslipidemia, glucose imbalance, the inability to maintain weight loss, insulin resistance, a cardiovascular disorder, memory loss, drug dependence, a depressive disorder, a panic disorder, an obsessive-compulsive disorder, anxiety, post-traumatic stress syndrome, and any other condition in which it is beneficial to inhibit, inversely agonize or modulate a cannabinoid receptor are described.