📜间羟基苯甲醛置于sodium Hydroxide体系中,用 甲醇,甲苯 作为反应溶剂,化学反应 8.0H,反应生成 间-香豆酸 参考文献:Synthesis Of Some Phenylpropanoid Glycosides (Ppgs) And Their Acetylcholinesterase/xanthine Oxidase Inhibitory Activities 标题:Synthesis Of Some Phenylpropanoid Glycosides (Ppgs) And Their Acetylcholinesterase/xanthine Oxidase Inhibitory Activities 摘要:在这项研究中,设计和合成了三类苯丙素糖苷(ppgs),以从红景天中分离的ppgs作为先导化合物.同时测试了它们对乙酰胆碱酯酶(ache)和黄嘌呤氧化酶(xod)的抑制能力.部分合成ppgs表现出了优异的酶抑制能力. DOI:10.3390/molecules16053580
专利号:US-2013150622-A1 优先权日:2011-12-12 标题:Stereoselective synthesis of tapentadol and its salts 发明人:FANDRICK DANIEL ROBERT; RODRIGUEZ SONIA; YANG BING-SHIOU 权利人:BOEHRINGER INGELHEIM INT; BOEHRINGER INGELHEIM INT 摘要:A process for the synthesis of a salt of tapentadol.
专利号:WO-2012089181-A1 优先权日:2010-12-30 标题 :O-substituted (2r,3r)-3-(3-hydroxyphenyl)-2-methyl-4-pentenoic acids and a method of obtaining the same 发明人:VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 权利人:ZENTIVA KS; VLASAKOVA RUZENA; HAJICEK JOSEF; ZEZULA JOSEF 摘要:The compounds of general formula II are new and represent important intermediates in the synthesis of tapentadol. In the synthesis of tapentadol of formula I and its pharmaceutically acceptable salts, O-protected (2R,3R)-acids of general formula II, in step A, are reacted in an inert organic solvent with an activating agent, optionally in presence of a catalyst or a base; in step B, the obtained compounds of general formula V, wherein R has the above mentioned meaning and X stands for chlorine or alkoxycarbonyloxyl group O-CO-OR 1 or pivaloyloxyl O-CO-t-Bu group, wherein R 1 is methyl or ethyl, are reacted with dimethylamine or its salts optionally in presence of a base; in step C, the obtained N, N-dimethylamides of general formula VI, wherein R has the above mentioned meaning, are reduced by means of hydride agents in a suitable solvent; in step D, the produced alkeneamines of general formula VII, wherein R has the above mentioned meaning, are hydrogenated on a metal catalysts in a suitable solvent; and, finally, in step E, the produced alkaneamines of general formula VIII, wherein R has the above mentioned meaning, are O-dealkylated by means of dealkylating agents, and, if required, the obtained tapentadol is converted by the action of a pharmaceutically acceptable acid to respective salts, e.g. hydrochloride.
专利号:US-6180830-B1 优先权日:1995-11-08 标题 :Method for preparing a bimetallic ruthenium/tin catalyst and a process for the synthesis of aldehydes 发明人:JACQUOT ROLAND 权利人:RHODIA CHIMIE SA 摘要:The present invention relates to a new process for the preparation of a bimetallic ruthenium/tin catalyst. The process for the preparation of a bimetallic ruthenium/tin catalyst according to the invention is characterised by the fact that it consists in carrying out the reduction of a ruthenium complex having an electrovalency of -4 and a coordination number of 6, the ligands being either a halogen atom or an anion or a tin halide. The catalyst is further employed for the preparation of aldehydes by reduction, in the vapor phase, of carboxylic acids, esters and anhydrides.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
参考文献:10.1021/jf0609882 摘要:Hsu CL, Huang SL, Yen GC. Inhibitory effect of phenolic acids on the proliferation of 3T3-L1 preadipocytes in relation to their antioxidant activity. J Agric Food Chem. 2006 Jun 14;54(12):4191–7. doi: 10.1021/jf0609882. 参考文献:10.1007/s00394-004-0482-2|10.1007/s00394-004-0524-9 摘要:Baba S, Osakabe N, Natsume M, Yasuda A, Muto Y, Hiyoshi T, Takano H, Yoshikawa T, Terao J. Absorption, metabolism, degradation and urinary excretion of rosmarinic acid after intake of Perilla frutescens extract in humans. European Journal of Nutrition. 2004 Feb 18;44(1):1–9. doi: 10.1007/s00394-004-0482-2.