CAS: 29122-68-7; Atenolol

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CAS号29122-69-8 4-(环氧乙基甲氧基)苯乙酰胺 | CAS号75-31-0 异丙胺 | CAS号29277-73-4 2-[4-[2-hydroxy... | CAS号623-05-2 对羟基苯甲醇 | CAS号14191-95-8 对羟基苯乙腈 | CAS号17194-82-0 对羟基苯乙酰胺 | CAS号35198-42-6 4-(2-Oxiranylme... | CAS号56715-13-0 (R)-(+)-阿替洛尔 | CAS号93379-54-5 (S)-(-)-阿替洛尔 | CAS号4747-21-1 N-甲基异丙胺 | CAS号52299-08-8 2-[4-(carboxyme...

4-羟基苯乙酰胺置于potassium Carbonate体系中,用 N,N-二甲基甲酰胺,丙酮 用作溶剂,化学反应 48.0H,反应生成阿替洛尔
参考文献:伯胺在溶剂指导下的环氧开环反应,用于合成β-氨基醇
标题:伯胺在溶剂指导下的环氧开环反应,用于合成β-氨基醇
摘要:摘要 据报道,在没有任何催化剂的情况下,可以由多种环氧化物和伯直链伯胺高效合成β-氨基醇,从而具有高收率和区域选择性.多种极性混合溶剂体系允许仲氨基醇相对于叔氨基醇的选择性形成.反应范围扩展到各种带有复杂官能团的芳族和脂族取代的环氧化物和伯胺. 据报道,在没有任何催化剂的情况下,可以由多种环氧化物和伯直链伯胺高效合成β-氨基醇,从而具有高收率和区域选择性.多种极性混合溶剂体系允许仲氨基醇相对于叔氨基醇的选择性形成.反应范围扩展到各种带有复杂官能团的芳族和脂族取代的环氧化物和伯胺.
Doi:10.1055/s-0036-1588356

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-2011024039-A1
优先权日:2009-08-25
标题 :Synthesis of novel 5-(2-(phenylsulfonyl)ethyl)-1h-indole derivatives
发明人：POTLURI RAMESH BABU; KODALI HARI PRASAD; VENTURI SRINIVASA RAO; TADIMALLA VENKATA SRIHARI
权利人:POTLURI RAMESH BABU; KODALI HARI PRASAD; VENTURI SRINIVASA RAO; TADIMALLA VENKATA SRIHARI
摘要:An objective of the present invention is to develop commercially viable methods for the synthesis of 5-[2-phenylsulfony)ethyl]-1H-indole of Formule (II), where R 1 and R 2 are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (II). Another objective of the present invention is to convert the product Formula (II) to Formula (I) in high yields, where R 1 and R 2 are same or different and each independently represent a hydrogen, fluorine, or di(lower alkyl)amino, acyl, or alkoxy carbonyl or chlorine atom, or a lower alkyl, lower alkoxy, nitro, cyano, aminolower alkylamine group Formula (I). One of the first processes attempted was by reacting the indole derivative of Formula (III) with aryl vinyl sulphones of Formula (V) as shown in Scheme-III. Another process attempted was by reacting the aniline derivative of Formula (VI) with aryl sulphones of Formula (VII) as shown in Scheme-III. Scheme IV.

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-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-2003050305-A1
优先权日:2000-05-22
标题:Thromboxane inhibitors, compositions and methods of use
发明人：TEJADA INIGO SAENZ DE
摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, 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 vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.