CAS: 101469-92-5; (S)-Tert-Butyl 3-Hydroxypyrrolidine-1-Carboxylate

上下游产品

tert-butyl dicarbonatedi-tert-butyl dicarbonate (3S)-1-benzyl-3-hydroxypyrrolidine-2,5-dione 3-hydroxypyrrolidine (S)-N-benzyl-3-hydroxypyrrolidine(S)-tert-butyl 3-(methylsulfonyloxy)pyrrolidine-1-carboxylate (3S)-N-(tert-butyloxycarbonyl)-3-(benzyloxy)pyrrolidine (R)-3-(5-bromo-pyridin-3-yloxy)-pyrrolidine-1-carboxylic acid tert-butyl ester tert-butyl (3R)-3-[4-(2-ethoxy-2-oxoacetyl)phenoxy]-1-pyrrolidinecarboxylate

(S)-N-Tert-Butoxycarbonylpyrrolidin-3-Yl Benzoate置于sodium Hydroxide体系中,用 甲醇 用作溶剂,化学反应 1.0H,以90%的收率获得(S)-1-N-叔丁氧羰基-3-羟基吡咯烷
参考文献:Synthesis Of Piperidinyl And Pyrrolidinyl Butyrates For Potentialin Vivo Measurement Of Cerebral Butyrylcholinesterase Activity
标题:Synthesis Of Piperidinyl And Pyrrolidinyl Butyrates For Potentialin Vivo Measurement Of Cerebral Butyrylcholinesterase Activity
摘要:阿尔茨海默病患者的尸检大脑中的生化变化包括乙酰胆碱酯酶(ache)和胆碱乙酰转移酶(chat)活性降低,表明中枢胆碱能系统活动减少,而丁酰胆碱酯酶(bche)活性增加.一种可以在活体中测量大脑区域性bche活性的方法可能对研究bche与阿尔茨海默病之间的关系非常有用.合成了七种化合物,分别为哌啶基或吡咯烷基丁酸酯,作为bche底物放射性示踪剂,通过正电子发射断层扫描(pet)映射中枢bche活性.用14C标记的化合物进行了测定,以确定它们被bche水解的速率和分配系数.这五种第二醇酯具有足够的亲脂性,可以轻松通过血脑屏障,而其代谢物具有足够的亲水性,可以在大脑中被保留.这些酯被bche水解的速率适中,并对bche相对于乙酰胆碱酯酶具有较高的特异性,而两种初级醇的酯水解得过于迅速,无法可靠估计局部大脑bche活性.根据这些结果,我们得出结论,当这些五种酯中的一种或多种用11C标记时,将是通过pet定量bche活性的有用示踪剂.版权©2001 John Wiley & Sons,Ltd.
Doi:10.1002/jlcr.429

专利信息

专利号:US-8399502-B2
优先权日:2008-09-17
标 题 :Analogs of indole-3-carbinol and their use as agents against infection
发明人：JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN
权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT
摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

专利号:US-2022363662-A1
优先权日:2021-04-20
标题 :Compounds as lxr agonists
发明人：PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V
权利人:INTEGRAL BIOSCIENCES PRIVATED LTD
摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.

专利号:US-8030501-B2
优先权日:2006-07-28
标题 :Process for producing optically active 3-amino nitrogen-containing compounds
发明人：OHNUKI MASATOSHI; IZUMIDA MASASHI; NISHIYAMA AKIRA; MATSUMOTO SHINGO
权利人:KANEKA CORP
摘要:Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr.

专利号:EP-1836163-B1
优先权日:2004-12-23
标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin
发明人：BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER
权利人:NOVARTIS AG
摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

专利号:US-7615634-B2
优先权日:2003-02-10
标题:4-aminopyrimidine-5-one derivatives
发明人：BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL
权利人:HOFFMANN LA ROCHE
摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.

专利号:CN-113025588-A
优先权日:2021-03-30
标 题 :An alcohol dehydrogenase KpADH mutant capable of catalyzing the synthesis of piperidine compounds