专利号:US-9567308-B1 优先权日:2015-07-23 标 题:Process for the synthesis of chlorzoxazone 发明人:BOGOGNA LUIGI; CICIONE LAVINIA; BAROZZA ALESSANDRO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of chlorzoxazone (1) from 4-chloro-2-aminophenol and ethyl chloroformate in the presence of a base. n n n n n n n n n n The process is particularly advantageous because it uses ethyl chloroformate instead of triphosgene, a highly dangerous reagent that releases phosgene and must be handled with extremely strict procedures to guarantee the safety of operators in industrial facilities. n Ethyl chloroformate allows the possibility of working with a number of solvents, including water. n The yield and purity of the product obtained are very high.
专利号:US-6852759-B2 优先权日:2002-03-28 标 题:Process for the synthesis of trans-alkenoic acids, use thereof 发明人:GUPTA VISHWA NATH; BHARDWAJ VIKRAM; SINGH BHUPINDER; CHANDAN BAL KRISHAN; SURI KRISHAN AVTAR; SATTI NARESH KUMAR; SURI OM PARKASH; HANDA SUKHDEV SWAMI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a process for the preparation of trans-alkenoic acids of general formula CH 3 —(CH 2 )n—CHâ•?(CH 2 )mCO 2 H where n=4 to 9 m=8 to 16. More particularly, the present invention relates to a process for the preparation of trans-tetracos-15-enoic acid, which is a bioactive constituent possessing dose-related hepatoprotective activity. The present invention also relates to the use thereof for hepatoprotection.
专利号:US-2003009034-A1 优先权日:2001-03-22 标题 :Transition metal mediated process 发明人:WISHART NEIL; RITTER KURT 摘要:This invention relates to a transition metal mediated process for the preparation of optionally substituted 2-amino-benzoxazoles and or 2-amino-benzimidazoles, which are useful as therapeutic agents or as intermediates in the synthesis of therapeutic agents.
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-2003109714-A1 优先权日:2001-03-22 标题 :Transition metal mediated process 发明人:WISHART NEIL; RUDOLPH ALENA; RITTER KURT 摘要:This invention relates to a transition metal mediated process for the preparation of optionally substituted 2-amino-benzoxazoles and or 2-amino-benzimidazoles, which are useful as therapeutic agents or as intermediates in the synthesis of therapeutic agents.
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.
1: Yasuhara M, Levy G. Pharmacodynamics of zoxazolamine and chlorzoxazone in rats. Pharm Res. 1988 Jul;5(7):401-7.
合成参考文献
摘要:Schnürch, M.; Hämmerle, J.; Stanetty, P., Science of Synthesis Knowledge Updates, (2010) 1, 163. 摘要:Schnürch, M.; Hämmerle, J.; Stanetty, P., Science of Synthesis Knowledge Updates, (2010) 1, 192. 摘要:Archives Internationales de Pharmacodynamie et de Therapie., 128(112), 1960 [] 摘要:Federation Proceedings, Federation of American Societies for Experimental Biology., 16(319), 1957 参考文献:10.4269/ajtmh.1980.29.227 摘要:Cha YN, Heine HS, Bueding E. Effect of unisexual Schistosoma mansoni infections on hepatic drug metabolism of mice. Am J Trop Med Hyg. 1980 Mar;29(2):227–33. doi: 10.4269/ajtmh.1980.29.227.