📜N-乙氧羰基-4-哌啶酮置于氢氧化钾,溴代异丁烷,Magnesium体系中,用 乙醚,乙醇 作为反应溶剂,化学反应 13.0H,反应生成 4-羟基哌啶 参考文献:Butaclamol-Like Neuroleptic Agents: Synthesis Of 1-(11H-Dibenz[b,F]-1,4-Oxathiepin-11-yl)Methyl-4-Isobutylpiperidin-4-Ol And Of Some Related Compounds 标题:Butaclamol-Like Neuroleptic Agents: Synthesis Of 1-(11H-Dibenz[b,F]-1,4-Oxathiepin-11-yl)Methyl-4-Isobutylpiperidin-4-Ol And Of Some Related Compounds 摘要:1-(11-二苯并[b,F]-1,4-噁硫杂环庚-11-基)甲基-4-哌啶酮(xiii),经过四步从11-二苯并[b,F]-1,4-噁硫杂环庚-11-羧酸(viii)得到,经异丁基溴化镁处理后得到标题化合物v,同时还有大量的二级醇vi,即还原产物.描述了一系列三取代苄基苯基硫醚衍生物xviii-Xxiv,Xxvi-Xxxi的合成;这些化合物是制备11-二苯并[b,F]-1,4-噁硫杂环庚乙酸xvi和xvii的潜在中间体.对11-二苯并[b,F]-1,4-噁硫杂环庚(vii)进行氯甲基化和另外两个常规步骤得到一种酸,其结构被指定为xvi.化合物v是"噁硫异丁氯胺醇"的开放模型,与这一事实一致,它表现为一种神经阻滞剂:它增加了大鼠脑纹状体中多巴胺的周转和代谢,表现为3,4-二羟基苯乙酸水平显著升高. DOI:10.1135/cccc19851484
专利号:WO-2016120890-A1 优先权日:2015-01-30 标题 :An enantioselective process for the synthesis of (2s,4r)-4-hydroxypipecolic acid 发明人:SURYAVANSHI GURUNATH; KAMBLE ROHIT BALKRISHNA 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to an improved process for synthesis of 4-hydroxy pipecolic acid. The present invention relates to an improved enantioselective process for the synthesis of (2S,4R)-4-hydroxypipecolic acid via Co(III) (salen)-catalyzed two stereocentered Hydrolytic Kinetic Resolution (HKR) of racemic 1,3-azido epoxide with good yields and high optical purity without any protecting groups. 10 31
专利号:WO-2025136243-A1 优先权日:2023-12-20 标题:Mechanochemical synthesis of histamine h1-receptor antagonists 发明人:AYDONAT SIMAY; OZEL MERTCAN; YIGITBASI JOANNA MARIANNA; BAYTEKIN BILGE; COLACINO EVELINA 权利人:IHSAN DOGRAMACI BILKENT UNIV; CENTRE NAT RECH SCIENT 摘要:The present invention relates to mechanochemical synthesis of histamine antagonists which are benzhydryl ethers and unsymmetrically disubstitutes piperazines and salts thereof. Said antihistamine active pharmaceutical ingredients can be diphenhydramine hydrochloride, cyclizine hydrochloride and diphenylpyraline hydrochloride. These antihistamines are used in the treatment of allergies, hives, hay fever (allergic rhinitis), conjunctivitis, reactions to insect bites and sings, nausea, motion sickness, insomnia.
专利号:US-6803468-B2 优先权日:2000-08-29 标 题 :Process for the synthesis of n-(5-methylnicontinoyl)-4 hydroxypiperidine, a key intermediate of rupatadine 发明人:KUMAR YATENDRA; PRASAD MOHAN; SINGH SHAILENDRA KUMAR 权利人:RANBAXY LAB LTD 摘要:The present invention relates to an improved and industrially advantageous process for the preparation of N-(5-methylnicotinoyl)-4-hydroxypiperidine of Formula I, as shown in the accompanied drawings. This compound is a key intermediate for the synthesis of rupatadine, a potent dual antagonist of histamine and platelet-activating factor (PAF).
专利号:US-9695169-B2 优先权日:2012-05-31 标 题:Synthesis of heterocyclic compounds 发明人:IBRAHIM PRABHA N 权利人:PLEXXIKON INC 摘要:Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.
专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 388. 摘要:Sato, N., Science of Synthesis Knowledge Updates, (2011) 4, 316. 摘要:Xing, Y.-K.; Fang, P.; Wang, Z.-H.; Mei, T.-S., Science of Synthesis: Special Topics, (2021) 1, 138. 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 2004. Toxicity, Repellency of Phytotoxicity of 979 Chemicals to Birds, Mammals and Plants. Research Report No. 04-01. National Wildlife Research Center, Fort Collins, Colorado. 118 pp. 摘要:Mandal, R.; Garai, B.; Sundararaju, B., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 212.