专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:WO-2025098683-A1 优先权日:2023-11-10 标 题:Improved process for the synthesis of imepitoin 发明人:ESTEVEZ LORA RAÚL; GARCÃ?A RAMOS Ã?LVARO; MARTINEZ GRAU MARÃ?A Ã?NGELES 权利人:JUSTESA IMAGEN S A U 摘要:The present invention describes an improved process for the preparation of imepitoin by means of an efficient preparation of its intermediate 1-(4- chlorophenyl)imidazolidine-2,4-dione followed by condensation with morpholine in the presence of ammonium chloride. Particularly, the invention relates to a process which provides imepitoin in high yield by removing the water generated in the reaction using a continuous process to distil, dry and recirculate the dried morpholine back to the reactor. More particularly, the invention relates to a process that provides imepitoin with very high purity by a simple washing with toluene and water. Still more particularly, the invention relates to a cost-effective process that is scalable for industrial application.
专利号:EP-4553066-A1 优先权日:2023-11-10 标题 :Improved process for the synthesis of imepitoin
专利号:IT-202100000782-A1 优先权日:2021-01-18 标 题 :PROCESS FOR THE SYNTHESIS OF IMEPITOIN
专利号:EP-4277899-A1 优先权日:2021-01-18 标 题:Process for the synthesis of imepitoin
专利号:CN-101565391-A 优先权日:2009-05-18 标 题 :One-pot synthesis of N, N'-di (p-chlorophenyl) urea and preparation of 2, 4-dichloroaniline
1: Van Huis CA, Bigge CF, Casimiro-Garcia A, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Narasimhan LS, Schaum RP, Zhang E, Bryant JW, Haarer S, Janiczek N, Leadley RJ Jr, McClanahan T, Thomas Peterson J, Welch KM, Edmunds JJ. Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors. Chem Biol Drug Des. 2007 Jun;69(6):444-50. German.
合成参考文献
摘要:Aggarwal, P.; Bebbington, M. W. P., Science of Synthesis Knowledge Updates, (2012) 2, 474. 摘要:Wan, J.-P., Science of Synthesis: Multicomponent Reactions, (2013) 2, 378.