📜戊二酸二甲酯置于氯化亚砜,Potassium Hydroxide体系中,用 甲醇 用作溶剂,化学反应 5.0H,反应生成4-氯甲酰基丁酸甲酯 参考文献:Design,Synthesis And Preliminary Bioactivity Studies Of 1,3,4-Thiadiazole Hydroxamic Acid Derivatives As Novel Histone Deacetylase Inhibitors 标题:Design,Synthesis And Preliminary Bioactivity Studies Of 1,3,4-Thiadiazole Hydroxamic Acid Derivatives As Novel Histone Deacetylase Inhibitors 摘要:Histone Deacetylase (Hdac) Inhibitors Have Emerged As A New Class Of Anticancer Agents,Targeting The Biological Processes Including Cell Cycle,Apoptosis And Differentiation. In The Present Study,A Series Of 1,3,4-Thiadiazole Based Hydroxamic Acids Were Developed As Potent Hdac Inhibitors. Some Of Them Showed Good Inhibitory Activity In Hdac Enzyme Assay And Potent Growth Inhibition In Some Tumor Cell Lines. Among Them,Compound 6I (Ic50 = 0.089 Mu M),Exhibited Better Inhibitory Effect Compared With Saha (Ic50 = 0.15 Mu M). (C) 2012 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmc.2012.04.032
专利号:US-2010159540-A1 优先权日:2007-03-26 标题:Synthesis of resolvins and intermediates, compounds prepared thereby, and uses thereof 发明人:RODRIGUEZ ANA; SPUR BERND 权利人:RODRIGUEZ ANA; SPUR BERND 摘要:Methods are disclosed for the preparation of a new class of lipid mediators known as resolvins, with Resolvin D6 (4,17-dihydroxy-5E,7Z,10Z,13Z,15E,19Z-docosahexaenoic acid) being exemplary. Also disclosed are methods for the efficient synthesis of key intermediates in the preparation of such resolvins, such as isotopically labeled ω-3 fatty acid metabolites, and derivatives and analogs thereof. The invention likewise extends to the intermediates so prepared, and to the resolvins prepared with their use.
专利号:US-6107495-A 优先权日:1996-07-24 标题:Thienylcyclohexane derivatives for thienylcyclohexyl synthesis 发明人:CAZAUX JEAN-BERNARD; DAFNIET MICHEL; KAMENKA JEAN-MARC; MANGINOT ERIC 权利人:EXPANSIA SA 摘要:PCT No. PCT/FR97/01382 Sec. 371 Date Jan. 19, 1999 Sec. 102(e) Date Jan. 19, 1999 PCT Filed Jul. 24, 1997 PCT Pub. No. WO98/03498 PCT Pub. Date Jan. 29, 1998Novel thienylcyclohexane derivatives of general formula (I), wherein R' is the 2-thienyl or 3-thienyl radical, R is the cyano radical or a radical of formula -C(O)A, and R2'' is a saturated or unsaturated optionally cyclic hydrocarbon radical, or an aryl radical, are disclosed. Methods for preparing said compounds, and the use thereof as novel industrial products for the synthesis of thienylcyclohexyl derivatives, are also disclosed.
专利号:US-5216005-A 优先权日:1989-03-15 标题:Immunosuppressive analogues and derivatives of succinylacetone 发明人:NITECKI DANUTE E; ALDWIN LOIS; LEVENSON COREY H; MORELAND MARGARET; BRAUDE IRWIN; MARK DAVID F; RAPOPORT HENRY 权利人:CETUS CORP 摘要:Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: wherein n = 1-6 RIV = H, or alkyl and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
专利号:US-5173482-A 优先权日:1989-03-15 标 题 :Immunosuppressive analogues and derivatives of succinylacetone 发明人:NITECKI DANUTE E; MORELAND MARGARET; ALDWIN LOIS; LEVENSON COREY H; BRAUDE IRWIN; MARK DAVID F; RAPOPORT HENRY 权利人:CETUS CORP 摘要:Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: wherein n = 1-6 RIV = H, or alkyl and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
专利号:US-4895872-A 优先权日:1989-03-15 标题:Immunosupressive analogues and derivatives of succinylacetone 发明人:NITECKI DANUTE E; MORELAND MARGARET; ALDWIN LOIS; LEVENSON COREY H; BRAUDE IRWIN; MARK DAVID F; RAPAPORT HENRY 权利人:CETUS CORP 摘要:Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: wherein n = 1-6 RIV = H, or alkyl and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.
专利号:US-7442802-B2 优先权日:2002-06-27 标 题:Cyclooxygenase-2 selective inhibitors, compositions and methods of use 发明人:BANDARAGE UPUL K; EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; KHANAPURE SUBHASH P; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:NITROMED INC 摘要:The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated. The invention also provides methods for treating inflammation, pain and fever; for treating and/or improving the gastrointestinal properties of COX-2 selective inhibitors; for facilitating wound healing; for treating and/or preventing renal and/or respiratory toxicity; for treating and/or preventing other disorders resulting from elevated levels of cyclooxygenase-2; and for improving the cardiovascular profile of COX-2 selective inhibitors.
参考标题:Borane-Methyl Sulfide Reductive Cyclization Of ω-Ester Alkylamides: A Convenient Synthesis OfN-Substituted Cyclic Amines 作者:Michael C. Venuti,Oswald Ort 摘要:Borane-Methyl Sulfide (Bms) Reduction Of Variously N-Substituted Succinamic And Glutaramic Esters Affords The Corresponding N-Substituted Pyrrolidines And Piperidines In High Yields. The Limitations, Mainly Caused By Steric Hinderance Around The Amine Nitrogen, And Putative Intermediates Involved In This Conversion, As Detected By Incomplete Reaction And/or Synthesis Followed By Bms Reduction, Indicate That Cyclization And Amide Reduction Successfully Compete With Ester Reduction To Afford The N-Substituted Cyclized Amines.
合成参考文献
摘要:Park, K.; Jo, H., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 908. 摘要:Pitaval, A.; Echavarren, A. M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 566.