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-8076479-B2 优先权日:2006-08-28 标题 :Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates 发明人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI 权利人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI; SCHERING CORP 摘要:Disclosed is a process for the synthesis of compounds of Formula I n nby sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,n n nwherein R 1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R 2a —OH), R 2a is a linear, branched or cyclic alkyl group, R 2 is a linear, branched or cyclic alkyl group, and R 3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1,n n nwith a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.
专利号:WO-2024259491-A1 优先权日:2023-06-23 标 题:New synthesis method 发明人:FORD DANIEL; POZNAKS VIKTORS; FOTINS JURIS; ÄŒERÅ…AKS DMITRIJS 权利人:THE HEART RES INSTITUTE LTD 摘要:The present disclosure generally relates to a process for the synthesis of AZD6482. In particular, the present disclosure also relates to a process for the synthesis of enantiomerically pure AZD6482. The present disclosure also relates to a process for the synthesis of enantiomerically pure intermediates. The present disclosure also relates to compounds prepared by the processes and the use of such compounds to prepare compositions and to treat disorders.
专利号:US-2005215772-A1 优先权日:2002-08-19 标 题:Furanone derivatives and methods of making same 发明人:KUMAR NARESH 权利人:KUMAR NARESH 摘要:Novel synthesis methods, to the products of such novel methods, and to uses of these products. In particular, the present invention provides methods for the reactions of furanones, in particular fimbrolides, with amines. The invention has particular application in the synthesis of halogenated 1,5-dihydro-pyrrol-2-one, 5-halomethylene substituted 1,5-dihydropyrrol-2-ones (lactam analogues of fimbriolides), 5-amino substituted furanones and 5-aminomethylene-2(5H)-furanones and their synthetic analogues. The invention also relates to novel compounds and uses thereof.
专利号:WO-2025085030-A1 优先权日:2023-10-18 标 题:Synthesis of semisynthetic penicillin derivatives containing hydrazone-derived thiazolidine and imidazole ring 发明人:SARIPINAR EMIN; BURAN SUMEYYE 权利人:ERCIYES UNIV 摘要:The present invention relates to the novel semi-synthetic thiazolidine and imidazole penicillin, pharmaceutically acceptable derivatives thereof and their synthesis method that may cause biologically significant changes by the N-acylation reaction of 6-aminopenicillanic (6-APA) using new trisubstituted thiazolidine and imidazole acetyl chloride derivatives. The invention also relates to pharmaceutical compositions comprising these compounds and their use for therapeutic treatment in the human or animal body.
专利号:US-12358877-B2 优先权日:2019-03-05 标题:Synthesis of 4-amino-5-methyl-1H-pyridin-2(1H)-on (intermediate compound for the synthesis of the MR antagonist finerenone) from 2-chloro-5-methyl-4-nitro-pyridine-1-oxide using the intermediate compound 2-chloro-5-methyl-4-pyridinamine 发明人:PLATZEK JOHANNES; LOVIS KAI 权利人:BAYER AG; Bayer Pharma AG 摘要:The present invention relates to a novel and improved method for preparing 4-amino-5-methylpyridone of the formula (I)which is an intermediate in the preparation of the MR antagonist finerenone.
参考标题:Cyclooctyne [60]Fullerene Hexakis Adducts: A Globular Scaffold For Copper-Free Click Chemistry 作者:Javier Ramos-Soriano,José J. Reina,Alfonso Pérez-Sánchez,Beatriz M. Illescas,Javier Rojo,Nazario Martín 摘要:The Synthesis Of A New Highly Symmetric Hexakis Adduct Of C60 Appended With 12 Cyclooctyne Moieties Has Been Carried Out. This Compound Has Been Used For The Copper-Free Strain-Promoted Cycloaddition...