Pyrimidinium Chloride置于溴,Sodium Carbonate体系中,用 水,硝基苯,苯 作为反应溶剂,化学反应生成 5-溴嘧啶 参考文献:Process For Bromination Of Pyrimidine 标题:Process For Bromination Of Pyrimidine 摘要:用溴化物溴化嘧啶的过程包括在有机溶剂中,在该过程的条件下,高温下与嘧啶的氢卤化物加成盐反应.该过程还被证明适用于其他含氮杂环化合物.
专利信息
专利号:US-9981949-B2 优先权日:2008-12-01 标题 :Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:OYSTER POINT PHARMA INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, its salt forms, and novel polymorphic forms of these salts.
专利号:US-8604191-B2 优先权日:2008-12-01 标 题:Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3YLVINYL)pyrimidine 发明人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT 权利人:AKIREDDY SRINIVASA RAO; BHATTI BALWINDER SINGH; CUTHBERTSON TIMOTHY J; DULL GARY MAURICE; MILLER CRAIG HARRISON; MITCHENER JR JOSEPH PIKE; MUNOZ JULIO A; OTTEN PIETER ALBERT; TARGACEPT INC 摘要:The present invention relates to the stereospecific synthesis of (R)-5-((E)-2-pyrrolidin-3-yl)pyrimidine, novel salt forms, and novel polymorphic forms of these salts.
专利号:US-3869456-A 优先权日:1972-03-13 标 题 :Synthesis of 5-pyrimidinecarbinols 发明人:TAYLOR HAROLD M; DAVENPORT JAMES D; HACKLER RONALD E 权利人:LILLY CO ELI 摘要:There is disclosed an improved method of synthesizing 5pyrimidinecarbinols by the addition of an alkyllithium to a mixture of 5-halopyrimidine and a ketone at a low temperature. The product compounds are useful as plant fungicides and as plant growth regulators.
专利号:US-6288221-B1 优先权日:1998-08-20 标 题 :Methods of synthesis of halogen base-modified oligonucleotides and subsequent labeling with a metal-catalyzed reaction 发明人:GRINSTAFF MARK W; BEILSTEIN AMY E; KHAN SHOEB I 权利人:UNIV DUKE 摘要:The present invention provides metal-containing purines, pyrimidines, nucleosides, nucleotides and oligonucleotides; including phosphoramidite and photolabile derivatives thereof, including methods of making and method of using same. The present invention provides a method for detection of nucleic acid sequences via electrochemical or photochemical means.
专利号:US-RE37623-E 优先权日:1993-11-02 标题:Enzyme inhibitors, their synthesis, and methods for use 发明人:EL KOUNI MAHMOUD H; NAGUIB FARDOS N M; SCHINAZI RAYMOND F 权利人:EL KOUNI MAHMOUD H; NAGUIB FARDOS N M; SCHINAZI RAYMOND F 摘要:Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula n where X is S or Se; Y is H, I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R 1 is H or an acyclo tail having the general formula n where R 2 is H, CH 2 OH or CH 2 NH 2 ; R 3 is OH, NH 2 , or OCOCH 2 CH 2 CO 2 H; and R 4 is O, S, or CH 2 . n The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
[参考文献]: Xiaofeng Rao, Et Al. A Highly Efficient And Aerobic Protocol For The Synthesis Of N-Heteroaryl Substituted 9-Arylcarbazolyl Derivatives Via A Palladium-Catalyzed Ligand-Free Suzuki Reaction. Org Biomol Chem. 2012 Oct 21;10(39):7875-83.
合成参考文献
摘要:Shimizu, M., Science of Synthesis Knowledge Updates, (2010) 3, 41. 摘要:Lubell, W. D.; St-Cyr, D. J.; Dufour-Gallant, J.; Hopewell, R.; Boutard, N.; Kassem, T.; Dörr, A.; Zelli, R., Science of Synthesis Knowledge Updates, (2013) 1, 309. 摘要:Hou, X.-L.; Peng, X.-S.; Yeung, K.-S.; Wong, H. N. C., Science of Synthesis Knowledge Updates, (2011) 2, 297. 摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 100. 摘要:Kwiecień, H., Science of Synthesis Knowledge Updates, (2018) 3, 198.