1-[3-(Triphenylmethylthio)-2-Methylpropanoyl]-L-Proline Tert.Butyl Ester 以 苯甲醚,三氟乙酸 作为反应溶剂,化学反应 1.0H,以to Yield 1-[3-Mercapto-2-Methylpropanoyl]-L-Proline的收率获得产物卡托普利杂质8 参考文献:Proline Derivatives And Related Compounds 标题:Proline Derivatives And Related Compounds 摘要:新的脯氨酸衍生物及相关化合物具有一般式##str1##,可用作血管紧张素转换酶抑制剂.
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-8431712-B2 优先权日:2004-02-09 标 题 :Methods for the synthesis of pyridoxamine 发明人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT 权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC 摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.
专利号:US-6069248-A 优先权日:1998-08-21 标题 :Process for the synthesis of triazolopyridazine compounds 发明人:BOLDI ARMEN M; JOHNSON CHARLES R 权利人:AXYS PHARM INC 摘要:The present invention provides a process for the synthesis of triazolopyridazine based compounds represented by Formula A: ##STR1## These compounds have utility as angiotensin related antihypertensive agents.
专利号:WO-2023169082-A1 优先权日:2022-10-24 标 题:Synthesis method and application of benzothiadiazole-1-ketone compound and derivative thereof 发明人:YI WEI; ZHOU ZHI; WU LIEXIN 权利人:UNIV GUANGZHOU MEDICAL 摘要:Disclosed in the present invention are a synthesis method and application of a benzoselenazole-1-ketone compound and a derivative thereof. Sulfoximine and the element selenium are used as raw materials, and by means of a rhodium catalysis direct C-H functionalization reaction, synthesis of a series of benzoselenazole-1-ketone compounds is achieved. The solution has the advantages of strong functional group compatibility, wide substrate universality, mild conditions, simple operations, and high efficiency and universality. Meanwhile, sulfoximine and the element selenium are used as initial raw materials, a direct C-H functionalization reaction is carried out, and by means of chiral phosphoric acid, synthesis of the chiral benzoselenazole-1-ketone compound is achieved. The application prospect is good, and a sulfydryl structure in biomacromolecules such as polypeptides, saccharides, drug molecules and proteins can be specifically marked. Good anti-SARS-CoV-2 virus activity is exhibited, a trastuzumab biological conjugate can effectively image HER 2 receptors on the cell surface, displays strong fluorescence, and can be applied to the preparation of an imaging reagent for the HER 2 receptor on the cell surface.
1: Martínez-Aguilar L, Lezama-Martínez D, Orozco-Cortés NV, González-Espinosa C, Flores-Monroy J, Valencia-Hernández I. Antihypertensive properties of a the novel morphologic derivative (4-tert-buthyl-2,6-bis (thiomorpholine-4-ilmethyl)phenol). J Cardiovasc Pharmacol. 2015 Nov 11. [Epub ahead of print] doi: 10.1590/abd1806-4841.20153390. 3: Tang Y, Hu X, Lu X. Captopril, an angiotensin-converting enzyme inhibitor, possesses chondroprotective efficacy in a rat model of osteoarthritis through suppression local renin-angiotensin system. Int J Clin Exp Med. 2015 Aug 15;8(8):12584-92. eCollection 2015.
合成参考文献
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