1-乙酰基-4-苄基哌嗪置于palladium On Activated Charcoal 氢气体系中,用 甲醇 用作溶剂,化学反应生成1-乙酰哌嗪 参考文献:New Antiproliferative Benzoindolinothiazepines Derivatives 标题:New Antiproliferative Benzoindolinothiazepines Derivatives 摘要:New Benzoindolinothiazepines Containing A Piperazine Moiety Are Described As Potent Antiproliferative Agents Against Pc3 Human Prostatic Cell Lines. This Activity Could Be Explained By An Accumulation Of Cells In G1 Phase. (C) 2004 Elsevier Sas. All Rights Reserved. Doi:10.1016/j.Ejmech.2004.10.008
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:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:WO-2024137329-A1 优先权日:2022-12-20 标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
专利号:US-11702380-B2 优先权日:2021-03-10 标 题:Synthesis of omecamtiv mecarbil 发明人:CAILLE SEBASTIEN; MURRAY JAMES; QUASDORF KYLE; NGUYEN HANNAH; SILVA ELIPE MARIA VICTORIA; ERICSON ARI ELIZABETH 权利人:AMGEN INC 摘要:Provided herein are synthetic methods for the preparation of intermediates that are utilized in the synthesis of omecamtiv mecarbil dihydrochloride.
专利号:US-11779912-B2 优先权日:2016-10-19 标题 :Synthesis and characterization of Ru alkylidene complexes 发明人:JOHNS ADAM M; HERRON JESSICA R; PEDERSON RICHARD L; FIAMENGO BRYAN A; BEERMAN JENNIFER A; LIN TZU-PIN; CHU CRYSTAL K; GRUBBS ROBERT H 权利人:UMICORE AG & CO KG; CALIFORNIA INST OF TECHN 摘要:This invention relates generally to olefin metathesis catalyst compounds, to the preparation of such compounds, compositions comprising such compounds, methods of using such compounds, articles of manufacture comprising such compounds, and the use of such compounds in the metathesis of olefins and olefin compounds. The invention has utility in the fields of catalysts, organic synthesis, polymer chemistry, and industrial and fine chemicals industry.
专利号:US-6080860-A 优先权日:1992-08-31 标 题:Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor 发明人:KARIMIAN KHASHAYAR; MURTHY KESHAVA; HALL DARREN 权利人:BRANTFORD CHEMICALSS INC 摘要:Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
[参考文献]: Tarek Mohamed, Et Al. Development Of 2-Substituted-N-(Naphth-1-Ylmethyl) And N-Benzhydrylpyrimidin-4-Amines As Dual Cholinesterase And Aβ-Aggregation Inhibitors: Synthesis And Biological Evaluation. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5881-7. [参考文献]: Zu-Ping Wu, Et Al. Synthesis And Acetylcholinesterase And Butyrylcholinesterase Inhibitory Activities Of 7-Alkoxyl Substituted Indolizinoquinoline-5,12-Dione Derivatives. Arch Pharm (Weinheim). 2012 Mar;345(3):175-84.
合成参考文献
摘要:Huang, Y.; Dömling, A., Science of Synthesis: Multicomponent Reactions, (2013) 1, 261. 摘要:Tested as SID 174525510 in AID 781327: 摘要:Kiyokawa, K., Science of Synthesis: Hypervalent Halogens in Organic Synthesis, (2025) .