1-乙酰基-1H-苯并噻唑 以 N,N-二甲基甲酰胺 用作溶剂,化学反应生成N-乙酰苯胺 参考文献:Pedersen,Steen Uttrup; Lund,Henning,Acta Chemica Scandinavica. Series B: Organic Chemistry And Biochemistry,1988,Vol. 42,# 5,P. 319-323 标题:Pedersen,Steen Uttrup; Lund,Henning,Acta Chemica Scandinavica. Series B: Organic Chemistry And Biochemistry,1988,Vol. 42,# 5,P. 319-323
专利信息
专利号:US-7199257-B1 优先权日:1999-06-10 标题 :Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide 发明人:SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; BOR ADAM; DEMETER ADAM; TRISCHLER FERENC; HORVATH JANOS; BRLIK JANOS 权利人:RICHTER GEDEON VEGYESZET 摘要:A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.
专利号:US-10751419-B2 优先权日:2014-05-01 标题:Method for synthesis of reactive conjugate clusters 发明人:MIGAWA MICHAEL T; YU JINGHUA; WAN W BRAD; PATEL SAYTEN P; VASQUEZ GUILLERMO; KINBERGER GARTH A; PRAKASH THAZHA P; SETH PUNIT P; SWAYZE ERIC E 权利人:IONIS PHARMACEUTICALS INC 摘要:Provided herein are improved methods for the synthesis of reactive conjugate clusters and intermediates used in such methods. In particular, improvements are provided that enhance the synthesis of reactive conjugate clusters by reducing the number of synthetic steps required. The reactive conjugate clusters prepared using the improved methods don't include any transacylation impurities that are formed using existing methods. The improved methods also provide an increase in overall yield and a cost benefit over existing methods.
专利号:US-8901352-B2 优先权日:2011-01-13 标题 :Method for the synthesis of rasagiline 发明人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN 权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S 摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.
专利号:WO-9407900-A1 优先权日:1992-09-25 标 题 :Synthesis of n-glycosylated compounds with the use of a mild, iodine-catalyzed reaction 发明人:KOREEDA MASATO; HOUSTON TODD A 权利人:UNIV MICHIGAN 摘要:The invention concerns N-glycosylated derivatives of nitrogen nucleophile compounds. The invention also concerns a mild, cost effective, stereoselective, regioselective, and generally applicable method for the preparation of N-glycosides by N-glycosylation of azide and amide nucleophile compounds. The method employs iodine in a catalytic amount that uniquely does not pose an environmental hazard. The invention provides efficient access to key intermediates for the synthesis inter alia of analogs of AZT and DDI and for the synthesis of conventional N-nucleoside antibiotic drugs and their novel N-glycosylated analogs.
专利号:US-5545568-A 优先权日:1992-09-14 标题:Solid phase and combinatorial synthesis of compounds on a solid support 发明人:ELLMAN JONATHAN A 权利人:UNIV CALIFORNIA 摘要:Methods, compositions, and devices for synthesizing combinatorial libraries of various useful compounds, such as benzodiazepines, prostaglandins, β-turn mimetics and glycerol-derived drugs is described. In order to expediently synthesize such combinatorial libraries of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. This disclosure thus also describes an important extension of solid phase synthesis methods to nonpolymeric organic compounds.
专利号:US-5919969-A 优先权日:1996-06-05 标 题 :Synthesis of yellow couplers 发明人:CRAWLEY MICHAEL W 权利人:EASTMAN KODAK CO 摘要:The invention provides a method of synthesis of a image-dye forming coupler of formula (I) wherein X is a substituent linked to the coupler by an atom of oxygen, sulfur or nitrogen R1 is an alkyl or aryl group, R2 is a hydrogen atom or an alkyl group; R3 to R7 are the same or different and selected from a hydrogen atom and substituent groups; which method comprises the reaction of a compound of formula (II) wherein R and R1 are the same or different and are as defined above for R1 and X is as defined above with a compound of formula (III) wherein R2 to R7 are as defined above, in the presence of an inert organic solvent.
参考文献:10.1007/s00894-011-1156-7 摘要:Roohi H, Moghadam B. Proton transfer from H2O to p-substituted anilide anion: can the size of water cluster influence the N-⋅⋅⋅H–OH→N–H⋅⋅⋅OH- switching. Journal of Molecular Modeling. 2011 Jul 12;18(4):1313–24. doi: 10.1007/s00894-011-1156-7. 参考文献:10.1007/s00572-011-0399-6 摘要:Cosme M, Stout MJ, Wurst S. Effect of arbuscular mycorrhizal fungi (Glomus intraradices) on the oviposition of rice water weevil (Lissorhoptrus oryzophilus). Mycorrhiza. 2011 Oct;21(7):651–8. doi: 10.1007/s00572-011-0399-6. 参考文献:10.1371/journal.pone.0022194 摘要:Lorrain A, Argüelles J, Alegre A, Bertrand A, Munaron J, Richard P, Cherel Y. Sequential Isotopic Signature Along Gladius Highlights Contrasted Individual Foraging Strategies of Jumbo Squid (Dosidicus gigas). PLoS ONE. 2011 Jul 14;6(7):e22194. doi: 10.1371/journal.pone.0022194.