2-(2-Chlorobenzylidene)Malonic Acid 反应生成 邻氯肉桂酸 参考文献:Stuart,Journal Of The Chemical Society,1888,Vol. 53,P. 143 标题:Stuart,Journal Of The Chemical Society,1888,Vol. 53,P. 143
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-9085605-B2 优先权日:2010-05-27 标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate 发明人:LIU GANG; ZHAO NAN; MA YAO 权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD 摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.
专利号:US-6562844-B2 优先权日:1998-01-23 标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-7002020-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:CN-116411294-A 优先权日:2021-12-31 标题:Method for electrochemical synthesis of p-chlorobenzaldehyde
专利号:EP-3239139-B1 优先权日:2010-05-27 标题 :Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 201. 摘要:Nguyen, B. N.; Hii, K. K.; Szymański, W.; Janssen, D. B., Science of Synthesis: Stereoselective Synthesis, (2011) 1, 643. 摘要:Bartsch, S.; Vogel, A., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 302. 摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 387. 摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 385.