2-Ethanesulfonyl-4-Chloro-6-Methyl-Pyrimidine置于氨体系中,化学反应生成 2-氨基-4-氯-6-甲基嘧啶 参考文献:Researches On Pyrimidines. Clviii. The Oxidation Of Mercaptopyrimidines With Chlorine Water 标题:Researches On Pyrimidines. Clviii. The Oxidation Of Mercaptopyrimidines With Chlorine Water 摘要: DOI:10.1021/ja01274A029
专利信息
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-8853228-B2 优先权日:2007-06-04 标 题:Heterocyclic analogs of propargyl-linked inhibitors of dihydrofolate reductase 发明人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE 权利人:ANDERSON AMY C; WRIGHT DENNIS L; FREY KATHLEEN MARY; PAULSEN JANET LEIGH; SCOCCHERA ERIC WILLIAM; VISWANATHAN KISHORE; UNIV CONNECTICUT 摘要:The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
专利号:US-2011124634-A1 优先权日:2008-05-13 标 题:Bioactive compounds for treatment of cancer and neurodegenerative diseases 发明人:SUN CONNIE L; LI XIAOYUAN 权利人:PONIARD PHARMACEUTICALS INC 摘要:The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.
专利号:US-8426432-B2 优先权日:2007-06-04 标 题 :Inhibitors of dihydrofolate reductase with antibacterial antiprotozoal, antifungal and anticancer properties 发明人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO 权利人:ANDERSON AMY C; WRIGHT DENNIS L; PELPHREY PHILLIP M; JOSKA TAMMY M; BOLSTAD ERIN S D; BOLSTAD DAVID B; POPOV VELJKO; UNIV CONNECTICUT 摘要:The compositions and methods described herein discloses the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus , fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii . These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-7002020-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
[参考文献]: Christer B Aakery, Et Al. Co-Crystal Screening Of Diclofenac. Pharmaceutics. 2011 Aug 31;3(3):601-14. [参考文献]: T Jayavarthanan, Et Al. Vibrational Spectra, Uv And Nmr, First Order Hyperpolarizability And Homo-Lumo Analysis Of 2-Amino-4-Chloro-6-Methylpyrimidine. Spectrochim Acta A Mol Biomol Spectrosc. 2012 Nov:97:811-24.
合成参考文献
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 354. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 376. 摘要:Molander, G. A.; Ryu, D., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 31.