CAS: 36894-69-6; Labetalol

上下游产品

1-phenyl-3-butanol 5-(2-bromoacetyl)-2-hydroxybenzamide acetyl>benzamide2-hydroxy-5-acetylbenzamide labetaol(RS)-1-methyl-3-phenylpropylamine 5-formyl-2-hydroxy-benzamide (S,R)-labetalol *)>-2-hydroxy-5-ethyl>benzamide*)-2-hydroxy-5-1-hydroxy-2-(1-methyl-3-phenylpropyl)aminoethylbenzamide

4-苯基-2-丁醇置于palladium 10% On Activated Carbon,氢气,Potassium Carbonate,三乙胺体系中,用 甲醇,二氯甲烷,乙腈 用作溶剂,-10.0~81.0 °C,500.01 Kpa 条件下,反应 8.0H,反应生成拉贝洛尔
参考文献:一种盐酸拉贝洛尔的制备方法
标题:一种盐酸拉贝洛尔的制备方法
摘要:本发明提供了一种盐酸拉贝洛尔的制备方法,属于医药技术领域.本发明提供的制备方法,以5‑卤代乙酰基水杨酰胺作为起始原料与苄胺进行亲核取代反应,然后与3‑卤代丁基苯进行亲核取代反应(或者是与3‑羟基丁基苯和对甲基苯磺酰氯酯化反应产物进行胺酯交换反应),再进行催化氢化反应反应后成盐,得到盐酸拉贝洛尔.本发明提供的制备方法,采用苄胺替代二苄胺,原料的原子利用率高,对环境友好,体现了绿色化学的原子经济性;胺酯交换反应选择性高,所得产物直接用于下一步反应;采用一步法脱除保护剂和还原羰基缩短了工艺路线;制备方法操作简便且稳定性和可控性高,生产成本高,产率高,适宜工业化生产.

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-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-5442118-A
优先权日:1994-04-22
标题 :Asymmetric synthesis of (R)- and (S)-arylethanolamines from iminoketones
发明人：GAO YUN; HONG YAPING; ZEPP CHARLES M
权利人:SEPRACOR INC
摘要:A method for the enantioselective reduction of an alpha -iminoketone to an alpha -aminoalcohol is disclosed. The method utilizes a borane reducing agent as the reducing agent and a chiral 1,3,2-oxazaborole as the catalyst. The method is applied to the synthesis of R-albuterol from methyl 5-acetylsalicylate in high yield and high optical purity.

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-2006000773-A1
优先权日:2003-03-07
标题:Process for the synthesis of a chromatographic phase
发明人：GLENNON JEREMY; HEALY LIAM
权利人:GLENNON JEREMY; HEALY LIAM
摘要:A process for the synthesis, delivery or deposition or localisation of a chromatographic phase, especially for chromatographic separation or solid phase extraction, comprises introducing a chemical moiety to a support using a supercritical fluid such as supercritical carbon dioxide.