3-溴咪唑[1,2-A]嘧啶置于sodium Tetrahydroborate,四甲基乙二胺,Palladium Diacetate,三苯基膦体系中,用 四氢呋喃 用作溶剂,化学反应 2.0H,以83%的收率获得咪唑并[1,2-A]吡啶 参考文献:Nabh4-Tmeda And A Palladium Catalyst As Efficient Regio-And Chemoselective System For The Hydrodehalogenation Of Halogenated Heterocycles 标题:Nabh4-Tmeda And A Palladium Catalyst As Efficient Regio-And Chemoselective System For The Hydrodehalogenation Of Halogenated Heterocycles 摘要: Doi:10.1016/j.Molcata.2014.06.012
专利号:WO-2024062080-A1 优先权日:2022-09-21 标题:Improved synthesis of psilocybin derivatives 发明人:HAMMES CHRISTIAN; STÖCKLI STEFAN 权利人:CARBOGEN AMCIS AG; AAMANYA AG 摘要:The present invention relates to an improved synthesis of psilocybin and alkyl- derivatives of psilocybin such as ethocybin (4-phosphoryloxy-N,N-diethyltryptamine, also known as phosphoryloxy-DET, PO-DET or CEY-39) and furthermore, relates to intermediates useful in the synthesis of these compounds.
专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-7179919-B2 优先权日:2004-03-18 标 题 :Stereoselective synthesis of certain trifluoromethyl-substituted alcohols 发明人:SONG JINHUA J; TAN ZHULIN; YEE NATHAN K; SENANAYAKE CHRIS HUGH; XU JINGHUA; GALLOU FABRICE 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:A process for stereoselective synthesis of a compound of Formula (I) n nwherein R 1 , R 2 , R 3 , R 4 , and R 5 are as described herein.
专利号:US-2006167025-A1 优先权日:2004-12-22 标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs 发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID 摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.
专利号:US-6127515-A 优先权日:1997-11-18 标 题:Functionalized resin for the synthesis of amides and peptides 发明人:MANFRE FRANCO; VANASSE BENOIT J; LABAUDINIERE RICHARD F; MORTON GEORGE C 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a functionalized amino resin of formula ##STR1## wherein S is a solid support; R is H or alkyl; A is ##STR2## Y is OH or OCOR 1 ; and R 1 is aliphatic or aromatic which is useful for the solid phase synthesis of amides, peptides and hydroxamic acids.
[参考文献]: Ahmed Kamal, Et Al. Efficient Solid-Phase Synthesis Of A Library Of Imidazo[参考文献]: George M Buckley, Et Al. Irak-4 Inhibitors. Part Iii: A Series Of Imidazo[参考文献]: Hao Yan, Et Al. One-Pot Three-Component Synthesis Of 3-Nitro-2-Arylimidazo[参考文献]: Huawen Huang, Et Al. Conversion Of Pyridine To Imidazo[参考文献]: Masahiko Hayakawa, Et Al. Synthesis And Biological Evaluation Of Imidazo[1,2-A]Pyridine Derivatives As Novel Pi3 Kinase P110Alpha Inhibitors. Bioorg Med Chem. 2007 Jan 1;15(1):403-12.
合成参考文献
参考文献:10.1107/s1600536811017077 摘要:Dahmani S, Kandri Rodi Y, Luis SV, Essassi el M, El Ammari L. Ethyl 8-amino-6-bromoimidazo[1,2-a]pyridine-2-carb-oxy-late. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1390. 参考文献:10.1016/j.bmcl.2011.06.090 摘要:Ducray R, Jones CD, Jung FH, Simpson I, Curwen J, Pass M. Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: Optimization of the aniline. Bioorganic & Medicinal Chemistry Letters. 2011 Aug;21(16):4702–4. doi: 10.1016/j.bmcl.2011.06.090.