专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-2008221303-A1 优先权日:2004-02-18 标 题:Method for the Preparation of Peptide-Oligonucleotide Conjugates 发明人:KATZHENDLER JEHOSHUA; KLAUZNER YAKIR; BEYLIS IRENA; MIZHIRITSKII MICHAEL; SHPERNAT YAACOV; ASHKENAZI BORIS; FRIDLAND DMITRI 权利人:KATZHENDLER JEHOSHUA; KLAUZNER YAKIR; BEYLIS IRENA; MIZHIRITSKII MICHAEL; SHPERNAT YAACOV; ASHKENAZI BORIS; FRIDLAND DMITRI 摘要:The present invention relates to the synthesis of peptide-oligonucleotide conjugates (POC). More specifically, the invention relates to a novel method for the preparation of peptide-oligonucleotide conjugates, which can be conducted under mild conditions on solid support, can be performed manually or by a synthesizer, can be used to synthesize alternating sequences of peptides and oligonucleotides, and is applicable to the synthesis of a wide variety of peptide-oligonucleotide conjugates constructed from alternate peptide and oligonucleotide blocks.
专利号:US-5115099-A 优先权日:1988-06-14 标 题:Substrates for determination of enzyme activity and intermediates for synthesis of the substrates as well as process for producing the intermediates 发明人:KUROIWA KATSUMASA; MATSUURA HITOSHI; KATAYAMA KATSUHIRO; NAKATSUYAMA SHUICHI; NAGASAWA TAKESHI; ENDO KOJI 权利人:NITTO BOSEKI CO LTD 摘要:Novel compounds represented by the following formula: ##STR1## wherein A represents a specific amino acid residue are excellent as substrates for determination of enzyme activity such as trypsin, etc. The compounds can be synthesized from novel arginyl-3-tert-alkyloxycarbonyl-4-nitroanilides by a novel process comprising a selective deprotection step whereby the protecting group on the α-amine group of arginine is removed in the presence of a hydrochloric acid, acetic acid and dimethylformamide mixture, but a tert-alkyl protecting group on the --COOH group of the nitroanilide ring is not removed by this step.
专利号:WO-0035868-A2 优先权日:1998-12-18 标 题:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives
专利号:EP-0513863-A1 优先权日:1988-06-14 标题:Substrates for determination of enzyme activity and intermediates for synthesis of the substrates as well as process for producing the intermediates
专利号:EP-0513863-B1 优先权日:1988-06-14 标题:Substrates for determination of enzyme activity and intermediates for synthesis of the substrates as well as process for producing the intermediates
[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:10.1080/14756366.2022.2070909 摘要:Kaur S, Nieto NS, McDonald P, Beck JR, Honzatko RB, Roy A, Nelson SW. Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase. Journal of Enzyme Inhibition and Medicinal Chemistry. 2022 May 05;37(1):1320–6. doi: 10.1080/14756366.2022.2070909.