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-7786156-B2 优先权日:2004-01-28 标 题 :Synthesis methods and intermediates for the manufacture of Rizatriptan 发明人:MARTIN PIERRE; BERENS ULRICH; BOUDIER ANDREAS; DOSENBACH OLIVER 权利人:RATIOPHARM GMBH 摘要:The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], n nor a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B]n n nwherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent.n n In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.
专利号:US-7250435-B2 优先权日:1999-10-20 标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n nthat are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G.n n This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:CN-120041848-A 优先权日:2025-02-18 标 题 :Method for electrochemically synthesizing chiral beta-ester nitrile and application of chiral beta-ester nitrile in synthesis of baclofen and rolipram
专利号:US-4803280-A 优先权日:1986-07-08 标题:Substituted 1,2,3-thia-diazole-4-thiolates 发明人:LEE VING J; CURRAN WILLIAM V 权利人:AMERICAN CYANAMID CO 摘要:Intermediates useful for synthesis of cephalosporins are disclosed, which intermediates are concerned with 1,2,3-thiadiazole-4-thiolates and the preparation of such thiolates.
专利号:FR-2628428-A1 优先权日:1988-03-09 标题:PROCESS FOR THE PREPARATION OF TRANSITION METAL COMPLEXES USEFUL AS RADIOPHARMACEUTICAL PRODUCTS OR FOR THE SYNTHESIS OF NEW RADIOPHARMACEUTICAL PRODUCTS
[参考文献]: R Paul, Et Al. Imidazo[参考文献]: Yu-Feng Li, Et Al. Methyl 3-(4-Methyl-Benzyl-Idene)Carbazate. Acta Crystallogr Sect E Struct Rep Online. 2010 May 22;66(Pt 6):O1429.
合成参考文献
摘要:Gnanaprakasam, B.; Chaudhari, M. B., Science of Synthesis Knowledge Updates, (2019) 2, 414. 摘要:Cormier, M.; Goddard, J.-P., Science of Synthesis, (2020) , 145. 摘要:Zhang, F.-G.; Ma, J.-A., Science of Synthesis: Knowledge Updates, (2025) 2. 摘要:Caron, S.; Lee, J.; Liu, Y.; Nguyen, T. N.; Piper, J. L.; Vicini, A. C., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2. 参考文献:10.1107/s1600536810033799 摘要:Lv LP, Liu S. (E)-Methyl 3-(3,5-dibromo-2-hy-droxy-benzyl-idene)carbazate. Acta Crystallogr Sect E Struct Rep Online. 2010 Aug 28;66(Pt 9):o2405.