专利号:US-6077962-A 优先权日:1998-12-24 标题 :N-3, 3-dimethylbutyl-L-aspartic acid and esters thereof, the process of preparing the same, and the process for preparing N-(N-(3,3-dimethylbutyl) -α L-aspartyl)-L- phenylalanine 1-methyl ester therefrom 发明人:PRAKASH INDRA; CHAPEAU MARIE-CHRISTINE D 权利人:NUTRASWEET CO 摘要:This invention relates to the chemical synthesis of N-[N-(3,3-dimethylbutyl)-L-α-aspartyl]-L-phenylalanine 1-methyl ester using peptide coupling methods. The coupling reaction is conducted by condensation of an activated derivative of novel N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester or by enzymatic coupling of N-neohexyl-L-aspartic acid with L-phenylalanine or L-phenylalanine methyl ester. This invention also relates to novel N-(3,3-dimethylbutyl)-L-aspartic acid, derivatives thereof and the preparation thereof. The activated derivative of N-neohexyl-L-aspartic acid may be an anhydride, mixed anhydride, active ester or an intermediate activated derivative thereof.
专利号:US-3891692-A 优先权日:1972-05-03 标题:N-(cyclopropylalkoxycarbonyl)amino acids 发明人:VEBER DANIEL F; BRADY STEPHEN F 权利人:MERCK & CO INC 摘要:Novel N-protected- Alpha -amino acid compounds are disclosed in which the amino functionality is protected by a cyclopropylmethoxycarbonyl or 1-cyclopropyl-ethoxycarbonyl. Processes for the synthesis of amino acids containing these protecting groups and the use of these novel amino acid compounds in the preparation of peptides are also disclosed.
专利号:US-3948971-A 优先权日:1972-05-03 标题 :N-protected-α-amino acid compounds 发明人:VEBER DANIEL F; BRADY STEPHEN F 权利人:MERCK & CO INC 摘要:Novel N-protected-α-amino acid compounds are disclosed in which the amino functionality is protected by a 1-methylcyclobutyloxycarbonyl or 1-methylcyclohexyloxycarbonyl. Processes for the synthesis of amino acids containing these protecting groups and the use of these novel amino acid compounds in the preparation of peptides are also disclosed.
专利号:WO-9221675-A1 优先权日:1991-06-03 标题:Synthesis of optically active lactones from l-aspartic acid and intermediates thereof
专利号:EP-0643710-A1 优先权日:1991-06-03 标 题 :Synthesis of optically active lactones from l-aspartic acid and intermediates thereof
专利号:US-5322942-A 优先权日:1991-06-03 标题 :Synthesis of optically active lactones from L-aspartic acid and intermediates thereof 发明人:RAPOPORT HENRY; DENER JEFFREY M; ZHANG LIN-HAU 权利人:UNIV CALIFORNIA 摘要:Optically active lactones are described, such as an intermediate lactone having the formula ##STR1## where R and R 2 are each independently alkyl with 1 to 6 carbon atoms, cycloalkyl with 6 to 10 carbon atoms, aryl with 6 to 10 carbon atoms, or arylalkyl with 7 to 19 carbon atoms, R 4 is H or C 1-6 alkyl, and Ar is a homo- or heteroaromatic ring with 5 or 6 ring atoms being optionally substituted by C 1-6 alkyl or alkoxy groups, halogen atoms, cyano or nitro groups. Such optically active, intermediate lactones are prepared from L-aspartic acid, and can be readily converted to (+)-pilocarpine and its analogues by hydrolysis, reduction, and hydrogenation, such as to an optically active lactone having the formula ##STR2## which is (+)-pilocarpine when R is ethyl, R 4 is H, and Ar is 1-methylimidazol-5-yl.
[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:10.1055/s-0029-1218267 摘要:Xie J, Maisonneuve S. One-Pot Synthesis of 1,4-Disubstituted 1,2,3-Triazoles from Aldehydes and Amines. Synlett. 2009 Oct 08;2009(18):2977–81. doi: 10.1055/s-0029-1218267.