N-苄基-N-甲酰基甘氨酸置于盐酸体系中,化学反应生成 N-苄基甘氨酸盐酸盐 参考文献:A Mild And Efficient Method For The One-Pot Monocarboxymethylation Of Primary Amines 标题:A Mild And Efficient Method For The One-Pot Monocarboxymethylation Of Primary Amines 摘要:本文介绍了一种在室温水溶液条件下进行伯胺单羧甲基化反应的温和而高效的方法.用两当量的乙醛酸处理各种伯胺的水溶液,可得到 N-甲酰基甘氨酸衍生物.直接水解粗反应溶液可得到胺一羧甲基化产物,收率从非常好到极佳. DOI:10.1055/s-2007-982531
专利号:EP-0535155-B1 优先权日:1990-06-14 标 题:Libraries of modified peptides with protease resistance 发明人:BARTLETT PAUL A; SANTI DANIEL; SIMON REYNA 权利人:CHIRON CORP; UNIV CALIFORNIA 摘要:Peptoids are provided which are polymers comprised of monomer units wherein the monomer units include at least some substitute amino acids and may include conventional amino acids. The peptoids can be synthesized in large numbers so as to provide libraries of peptoids which can be screened in order to isolate peptoids of desired biological activity. Certain peptoids are designed to mimic as closely as possible the activity of known proteins. Other peptoids are designed so as to have greater or lesser activity than known proteins and may be designed so as to block known receptor sites and/or elicit a desired immunogenic response and thereby act as vaccines. A range of different amino acid substitutes are disclosed, as are their methods of synthesis and methods of using such amino acid substitutes in the synthesis of peptoids and peptoid libraries. Methods of screening the libraries in order to obtain desired peptoids of a particular biological activity are also disclosed. The peptoids are preferably linked to a pharmaceutically active drug forming a conjugate with increased binding affinity to a particular biological receptor site.
专利号:WO-2011091548-A1 优先权日:2010-01-27 标 题:Method for cucurbitine synthesis 发明人:CHANG XIAOWEI; KHOSHDEL EZAT; PENG WEIMIN; WANG JINFANG; YAO YINFANG 权利人:UNILEVER PLC; UNILEVER NV; UNILEVER HINDUSTAN; CHANG XIAOWEI; KHOSHDEL EZAT; PENG WEIMIN; WANG JINFANG; YAO YINFANG 摘要:A method for the synthesis of cucurbitine comprising the step of forming a pyrrolidine ring by a 1,3 dipolar cycloaddition reaction.
专利号:US-6075121-A 优先权日:1990-05-15 标 题 :Modified peptide and peptide libraries with protease resistance, derivatives thereof and methods of producing and screening such 发明人:SIMON REYNA J; BARTLETT PAUL A; SANTI DANIEL V 权利人:CHIRON CORP 摘要:Peptoids are provided which are polymers comprised of monomer units wherein the monomer units include at least some substitute amino acids and may include conventional amino acids. The peptoids can be synthesized in large numbers so as to provide libraries of peptoids which can be screened in order to isolate peptoids of desired biological activity. Although the peptoids may include amino acids, they preferably include only substituted amino acids and are designed in a manner so as to have a particular biological activity. Certain peptoids are designed to mimic as closely as possible the activity of known proteins. Other peptoids are designed so as to have greater or lesser activity than known proteins and may be designed so as to block known receptor sites and/or elicit a desired immunogenic response and thereby act as vaccines. In that the peptoids are comprised of substitute amino acids they can be designed to have structures which natural proteins cannot conform to. A range of different amino acid substitutes are disclosed, as are their methods of synthesis and methods of using such amino acid substitutes in the synthesis of peptoids and peptoid libraries. Methods of screening the libraries in order to obtain desired peptoids of a particular biological activity are also disclosed. The peptoids are preferably linked to a pharmaceutically active drug forming a conjugate with increased binding affinity to a particular biological receptor site.
专利号:US-5532366-A 优先权日:1992-07-02 标 题:Heterocyclic amides 发明人:EDWARDS PHILIP D; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel amide derivatives which are pyrido[3,4-d]pyrimidin-7-ylacetamides which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these amide derivatives, processes for preparing the amide derivatives, pharmaceutical compositions containing such amide derivatives and methods for their use.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1007/s12274-023-6266-x 摘要:Wang H, Li L, Cao X, Zhen M, Wang C, Bai C. Application of mannose-modified fullerene immunomodulator selectively polarizes tumor-associated macrophages potentiating antitumor immunity. Nano Res. 2023 Nov;16(11):12855–63. doi: 10.1007/s12274-023-6266-x.