专利号:US-4962223-A 优先权日:1988-07-12 标题:Process for the synthesis of the levodopa 发明人:CANNATA VINCENZO; TAMERLANI GIANCARLO; MOROTTI MAURO 权利人:MINI RICERCA SCIENT TECNOLOG 摘要:New process for the synthesis of the levodopa, L-(-)-2-amino-3-(3,4-dihydyphenyl)propionic acid, drug used in the treatment of the Parkinson's disease. The process consists in resolving with d-camphorsulfonic acid, or with a salt thereof, the d,l-2-amino-3-(3,4-dimethoxyphenyl)propionitrile, obtained from the 3,4-dimethoxyphenylacetaldehyde, and in the subsequent hydrolysis and demethylation, by means of concentrated solutions of haloid acids, of the d-2-amino-3-(3,4-dimethoxyphenyl)propionitrile and of salts thereof.
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-2024084338-A1 优先权日:2022-11-22 标 题 :Recombinant Escherichia coli for producing rosmarinic acid and its application thereof 发明人:ZHOU JINGWEN; CHEN JIAN; WANG LIAN; ZENG WEIZHU; YU SHIQIN 权利人:UNIV JIANGNAN 摘要:The present disclosure discloses a recombinant Escherichia coli for producing rosmarinic acid and application thereof, belonging to the technical fields of genetic engineering and bioengineering. In the present disclosure, FjTA derived from Flavobacterium johnsoniae, endogenous hpaBC derived from E. coli, CbRAS derived from Coleus blumei, HPPR derived from Coleus scutellarioides, and Pc4CL1 derived from Petroselinum crispum are heterologously expressed in E. coli, realizing synthesis of rosmarinic acid. TcTAL derived from Trichosporon cutaneum and tyrC for removing feedback inhibition are introduced, further increasing synthesis throughput of caffeic acid, and PmLAAD derived from Proteus myxofaciens is heterologously expressed, realizing redistribution of L-DOPA. An endogenous gene menl is knocked out, improving the content and stability of a rosmarinic acid precursor. The recombinant strain constructed in the present disclosure can produce rosmarinic acid by fermentation at a yield of up to 511.2 mg/L, providing a new method for industrial production of rosmarinic acid.
专利号:US-8017786-B2 优先权日:2006-05-15 标 题:Substituted β-phenyl-α-hydroxy-propanoic acid, synthesis method and use thereof 发明人:ZHENG XIAOHUI; ZHANG QUNZHENG; WANG SHIXIANG; ZHAO XINFENG 权利人:UNIV NORTHWEST 摘要:The present invention relates to a compound of the formula (I), wherein R 1 , R 2 and R 3 are each independently selected from H, OH, F, Cl, Br, methoxy and ethoxy; or alternatively, R 1 and R 2 together form —OCH 2 O—, R 3 is selected from H, OH, methoxy, ethoxy and halogens; R 4 is OH or acyloxy; R 5 is cycloalkoxyl, amino and substituted amino, and when R 5 is selected from amino, at least one of R 1 , R 2 and R 3 is not H. The present invention further relates to a process for synthesizing a compound of the formula (I), and use of the compound of the formula (I) in the manufacture of a medicament for the prevention or treatment of cardiovascular or cerebrovascular diseases.
专利号:EP-4206236-A1 优先权日:2021-12-28 标题 :Compounds, their synthesis and compositions comprising the compounds for enhanced deposition of polymers onto hair surfaces 发明人:BREAKSPEAR STEVEN; NÖCKER BERND; WEITZEL JOHANNA; PAEZ JULIETA; PEARSON SAMUEL; BRÜCK STEFAN; CAMPO ARANZAZU DEL 权利人:KAO CORP 摘要:The present invention is on polymers derivatized with an organic deposition-enhancing group for their enhanced deposition onto keratin fibers, especially human hair. The deposition-enhancing group is a di-hydroxyl phenolic compound with a spacer alkyl group bound to a reactive amine or carboxyl group, which reacts with one of the hydroxyl, carboxyl, primary and secondary amine groups on the polymeric backbone. The invention is on the method of synthesizing such compounds and compositions comprising the compounds.
专利号:CN-203530178-U 优先权日:2013-08-29 标题 :Recovery device of excessive hydroquinone during synthesis of DHPPA (R-(+)-2-(4-hydroxyphenoxy) propionic acid
参考标题:Biosynthesis. Part 24. Speculative Incorporation Experiments With 1-Benzylisoquinolines And A Logical Approach Via C6-C2And C6-C3Precursors To The Biosynthesis Of Hasubanonine And Protostephanine 作者:Alan R. Battersby,Raymond C. F. Jones,Rymantas Kazlauskas,Craig W. Thornber,Somsak Ruchirawat,James Staunton 摘要:Many Possible 1-Benzyltetrahydroisoquinolines Have Been Examined As Possible Advanced Precursors Of The Alkaloids Hasubanonine (1) And Protostephanine (2) In Stephania Japonica Plants, But None Was Incorporated Significantly. Administration Of Various Precursor Molecules Having Only One Aromatic Ring, Such As Tyrosine, Has Demonstrated That Both Alkaloids Are Derived From Two Different C6-C2 Biogenetic
合成参考文献
摘要:Pollegioni, L.; Molla, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 277. 摘要:Herter, S.; Turner, N. J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 100. 参考文献:10.1016/s0022-3565(25)25984-5 摘要:Pogrund RS, Drell W, Clark WG. METABOLISM OF 3-HYDROXY- AND 3,4-DIHYDROXYPHENYLPYRUVIC ACIDS IN VIVO. The Journal of Pharmacology and Experimental Therapeutics. 1961 Mar;131(3):294–307. doi: 10.1016/s0022-3565(25)25984-5.