1,3-苯二醇单乙酸酯置于acyltransferase From Bacterium Pseudomonas Sp.Ygj3体系中,用 Aq. Phosphate Buffer,二甲基亚砜 用作溶剂,化学反应 36.0H,反应生成1,3-二乙酰氧基苯 参考文献:生物催化弗里德尔-克来福特酰化和弗里斯反应. 标题:生物催化弗里德尔-克来福特酰化和弗里斯反应. 摘要:弗里德尔-克来福特酰化通常用于芳基酮的合成,并且尚未引入可能受益于酶的化学和区域选择性的生物催化版本.这里描述的是一种细菌酰基转移酶,它可以催化缓冲液中酚类底物的 Friedel-Crafts C-酰化,而不需要 Coa 激活试剂.转化率高达 >99%,并且该酶接受各种 C-或 O-酰基供体,例如 Dapg 或乙酸异丙烯酯.此外,该酶能够使间苯二酚衍生物发生类似弗里斯重排的反应.这些发现为开发替代性和选择性 Cc 键形成方法开辟了道路. Doi:10.1002/anie.201703270
专利信息
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-2006128939-A1 优先权日:2004-12-03 标题 :One pot process for making polymeric antioxidants 发明人:KUMAR VIJAYENDRA; YANG SUIZHOU; CHOLLI ASHOK L 权利人:KUMAR VIJAYENDRA; YANG SUIZHOU; CHOLLI ASHOK L 摘要:Disclosed is a method for the synthesis of sterically hindered polymeric antioxidants based on phenol type antioxidant monomers. The method includes mono-deacetylating, polymerizing and deacetylating an aryl monomer represented by the following structural formula: n n nto produce a sterically hindered polymeric macromolecular antioxidant. X, R 10 and q are as defined herein. The disclosed method is a simple, direct and economical process for the synthesis of sterically hindered polymeric macromolecular antioxidants.
专利号:CN-108440553-A 优先权日:2018-03-16 标题 :A ruthenium complex catalyzed asymmetric synthesis of optically pure glabridin
专利号:GB-2355715-A 优先权日:1999-10-26 标 题 :Synthesis of Diamino- or triamino- 2,4,6- trinitrobenzene
专利号:GB-2355713-A 优先权日:1999-10-26 标题:Synthesis of Diamino-orTriamino- 2,4,6-trinitrobenzene
摘要:Journal of the American Pharmaceutical Association, Scientific Edition., 46(185), 1957 摘要:Marsini, M. A.; Pettus, T. R. R., Science of Synthesis, (2007) 31, 433.