L-亮氨酸,苯甲醇置于对甲苯磺酸,对甲苯磺酰氯体系中,用97%的收率获得l-亮氨酸苄酯对甲苯磺酸盐 参考文献:A Simple And Convenient Method For Esterification Of Tryptophan And Other Amino Acids 标题:A Simple And Convenient Method For Esterification Of Tryptophan And Other Amino Acids 摘要: Doi:10.1021/jo00149A024
专利号:US-2014213814-A1 优先权日:2011-06-16 标题:Process For Extraction Of Peptides And Its Application In Liquid Phase Peptide Synthesis 发明人:MONNAIE DIDIER; FORNI LUCIANO; GIRAUD MATHIEU 权利人:MONNAIE DIDIER; FORNI LUCIANO; GIRAUD MATHIEU; LONZA BRAINE S A; LONZA AG 摘要:A process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process includes a step a) and a step b): step a) including the addition of a component a1) and a component a2), whereby component a1) is toluene and component a2) is water, to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) including the subsequent separation of the organic layer containing the peptide from the aqueous layer. In an embodiment, a combination of toluene and an organic solvent 1 selected from n-heptane, 2-methyltetrahydrofuran, ethylacetate, isopropylacetate, acetonitrile and tetrahydrofuran is used for the process for extraction. The extraction step is preferably used in a process for preparation of a peptide in liquid phase.
专利号:US-4581167-A 优先权日:1982-01-19 标 题:Peptide synthesis and amino acid blocking agents 发明人:CARPINO LOUIS A; COHEN BERI 权利人:RESEARCH CORP 摘要:Process for the preparation of peptides including higher polypeptides utilizing indenylmethoxycarbonyl blocking groups and products produced thereby.
专利号:CN-114907229-A 优先权日:2021-02-07 标题:The preparation method of impurity in the synthesis of ubenimex
专利号:US-2014213759-A1 优先权日:2011-06-16 标题 :Process For Extraction Of Peptides And Its Application In Liquid Phase Peptide Synthesis
专利号:US-9861703-B2 优先权日:2013-06-07 标 题:Multi-targeted Ubenimex prodrug derivative and preparation method and use thereof 发明人:XU WENFANG; JIANG YUQI; ZHANG YINGJIE; ZOU MINGMING; HOU JINNING; LI JIN; WANG XUEJIAN; LI XIAOYANG 权利人:JINAN PLATINUM PHARMATECH CO LTD 摘要:The present invention relates to the design, synthesis, and biological study of multi-targeted Ubenimex pro-drug derivative. More particularly, provided in the present invention is a compound as shown by general structural formula (I) (wherein the definition of R is shown in the description). The derivative is a multi-targeted compound obtained by binding an aminopeptidase (APN/CD13) inhibitor, Ubenimex, with some anti-tumor drugs already on the market through an ester bond or amide bond, and is suitable for use as an anti-tumor drug for the treating various malignant tumors, and is especially suitable for treating various solid tumors.
专利号:US-6858585-B1 优先权日:1996-06-25 标题 :Cyclic depsipeptides and drugs containing the same as the active ingredient 发明人:YANAI MAKOTO; SUZUKI MASASHI; OSHIDA NORIO; KAWAMURA KOJI; HIRAMOTO SHIGERU; YASUDA ORIE; KINOSHITA NOBUHIRO; SHINGAI AKIKO; TAKASU MASAKO 权利人:NISSHIN SEIFUN GROUP INC 摘要:Cyclic depsipeptides represented by the formula n n nwherein:n n R is a straight or branched alkyl group of 5-20 carbon atoms or a straight or branched alkoxymethyl group of 5-15-carbon atoms; A, B, D, E and F independently each other are alanine, valine, leucine, isoleucine, phenylalanine, etc.; W and Z independently each other are aspartic acid, asparagine, glutamic acid or glutamine; and m and n independently each other is 0 or 1, or pharmacologically acceptable salts thereof. The present compounds are prepared according to a method conventionally used in peptide synthesis. The present compounds are useful as an agent for promoting the production of apolipoprotein E, a therapeutic agent for neurologic damages, a therapeutic agent for dementia, an agent for inhibiting the production of apolipoprotein B, an agent for promoting the production of apolipoprotein A1 or a therapeutic agent for hyperlipemia.