4-羟基-1-哌啶甲酸苄酯置于palladium On Activated Charcoal 氢气,三氧化硫吡啶,对甲苯磺酸,三乙胺体系中,用 甲醇,二甲基亚砜,乙酸乙酯,甲苯 用作溶剂,化学反应 121.0H,反应生成4-哌啶酮缩乙二醇 参考文献:Cooper,Curt S.; Klock,Pamela L.; Chu,Daniel T. W.,Journal Of Medicinal Chemistry,1992,Vol. 35,# 8,P. 1393-1398 标题:Cooper,Curt S.; Klock,Pamela L.; Chu,Daniel T. W.,Journal Of Medicinal Chemistry,1992,Vol. 35,# 8,P. 1393-1398
专利信息
专利号:US-10487070-B2 优先权日:2016-04-13 标 题:Process for preparing intermediates useful in the synthesis of antifungal drugs 发明人:BERTOLINI GIORGIO; COLLI CORRADO; SADA MARA; COLOMBO FEDERICA 权利人:OLON SPA; OLSON S P A 摘要:Subject-matter of the invention is a process for preparing intermediates useful in the synthesis of drugs, for example antifungal drugs, such as efinaconazole. Subject-matter of the invention are also such novel synthesis intermediates and the use thereof.
专利号:US-8859765-B2 优先权日:2011-11-30 标 题:Process for the manufacture of chiral catalysts and their salts 发明人:WU PING-YU; HENSCHKE JULIAN PAUL 权利人:SCINOPHARM TAIWAN LTD 摘要:The present invention provides efficient and economical methods for synthesis of (−)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.
专利号:US-8653282-B2 优先权日:2007-10-18 标 题:Preparation of dihydrothieno [3,2-D] pyrimidines and intermediates used therein 发明人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G 权利人:FRUTOS ROGELIO; KRISHNAMURTHY DHILEEPKUMAR; MULDER JASON ALAN; RODRIGUEZ SONIA; SENANAYAKE CHRIS HUGH; TAMPONE THOMAS G; BOEHRINGER INGELHEIM INT 摘要:The invention relates to improved methods of preparing dihydrothienopyrimidines of formula 1, and intermediates thereof, (I) wherein X is SO or SO 2 , preferably SO, and wherein R A , R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the description. The methods according to this invention are more suitable for large-scale synthesis of said compounds than prior methods because the new synthetic process avoids distillation and chromatographic purification between steps and results in a higher overall yield of the desired product.
专利号:US-9458111-B2 优先权日:2010-07-29 标题:Process for the synthesis of substituted urea compounds 发明人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS 权利人:LEARMONTH DAVID ALEXANDER; BROADBELT BRIAN; WAHNON JORGE BRUNO REIS; BIAL—PORTELA & CA S A 摘要:A process for preparing a substitute urea of Formula (II) or Formula (I), or a pharmaceutically acceptable salt or ester thereof: n nthe process comprising the reaction of a carbamate of Formula (II′): Formula (I′):n n nwith a primary or secondary amine of the formula R1R2NH, wherein ring A, and R1, R2, R5, V, W, X, Y and Z are as defined herein.
专利号:US-2005019747-A1 优先权日:2002-08-07 标 题 :Nanoliter-scale synthesis of arrayed biomaterials and screening thereof 发明人:ANDERSON DANIEL G; LEVENBERG SHULAMIT; LANGER ROBERT S 摘要:A method of screening cell-polymer interactions. The method includes depositing monomers as a plurality of discrete elements on a substrate, causing the deposited monomers to polymerize, thereby creating an array of discrete polymer elements on the substrate, incubating the substrate in a cell-containing culture medium, and characterizing a predetermined cell behavior on each polymer element.
专利号:US-11078163-B2 优先权日:2014-01-24 标 题 :Processes for the synthesis of substituted urea compounds 发明人:RUSSO DOMENICO; WAHNON JORGE BRUNO REIS; MATON WILLIAM; ESZENYI TIBOR 权利人:BIAL PORTELA & CA SA; BIAL PORTELA & Cª S A 摘要:The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, the process comprising the reaction of an imidazolyl intermediate of Formula IIa′ with a carbamoyl halide of the formula: R1R2NC(â•?O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa′ is prepared by oxidation of the derivative of R5 and R6, R6-C(â•?O)CH2R5 to form a glyoxal intermediate R6-C(â•?O)(Câ•?O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa′ and wherein the compound substituents are as defined herein.
摘要:Giel, M.-C.; Smedley, C. J.; Moses, J. E., Science of Synthesis, (2021) , 447. 摘要:Semeniuk, T.; Hamel, J.-D., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2.