CAS: 22839-61-8; (S)-2-Amino-4-(((S)-1-Methoxy-1-Oxo-3-Phenylpropan-2-yl)Amino)-4-Oxobutanoic Acid

相似化合物

186796-08-7 22839-47-0 13433-09-5

上下游产品

CAS号2577-90-4 (S)-2-氨基-3-苯基丙酸甲酯

📜L-苯丙氨酸甲酯置于钯 氢气,溶剂黄146体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应生成β-Asp-Phe甲基酯
参考文献:一些二肽的结构-味道关系.
标题:一些二肽的结构-味道关系.
摘要:
Doi:10.1021/ja01038A046

专利信息

专利号:US-4537714-A
优先权日:1982-07-20
标 题 :Process for the preparation of lower alkyl esters of N-L-α-aspartyl-L-phenylalanine and of new intermediates for their preparation
发明人：MUELLER HANS-RUDOLF; BOLLINGER HEINRICH
权利人:EPROVA AG
摘要:The invention relates to a selective process for the preparation of N-L-α-aspartyl-L-phenylalanine-1-lower alkyl ester which comprises: n A. reacting an L-aspartic acid 4-arylmethyl ester with a n (i) 1,3-diketone; or n (ii) acylacetic ester; n in the presence of a base to form the salt of n (i') L-N-(1-alkyl-2-acyl-vinyl)-aspartic acid 4-arylmethyl ester; or n (ii') L-N-(1-alkyl-2-alkoxycarbonyl-vinyl)-aspartic acid 4-arylmethyl ester, n and then either: n (1) reacting salt (i') or (ii') with an organic or inorganic acid halide having the formula X-A, wherein X represents a halogen and A has the meaning indicated hereinafter, or with an acid anhydride to form ##STR1## wherein R represents an alkyl radical with 1 to 6 carbon atoms; n R' represents an alkyl or alkoxy radical with 1 to 6 carbon atoms; n Ar represents the phenyl, nitrophenyl, halogenphenyl or alkylphenyl radical; and n A represents an acyl with 2 to 12 carbon atoms, alkoxycarbonyl with 2 to 12 carbon atoms, or a phosphoric acid, phosphorous acid, sulfuric acid, sulfurous acid or sulfonic acid radical; n and reacting ester (I) with an L-phenylalanine lower alkyl ester; or n (2) reacting a salt of (i') or (ii') with a phosphorazo-L-phenyl lower alkyl ester; to form n (i') N-L-α-N'-(1-alkyl-2-acyl-vinyl)-aspartyl-L-phenylalanine-1-lower alkyl-4-arylmethyl ester; or n (ii') N-L-α-N'-(1-alkyl-2-alkoxycarbonyl)aspartyl-L-phenylalanine-1-lower alkyl-4-arylmethyl ester; n B. reacting (i') or (ii') with a strong acid to split off the respective N-(1-alkyl-2-acyl-vinyl) or N-(1-alkyl-2-alkoxycarbonyl-vinyl) protective group and produce: n (iii) N-L-α-aspartyl-L-phenylalanine-1-lower alkyl-4-(arylmethyl)ester; and n C. subjecting ester (iii) to catalytic hydrogenation to selectively split off the 4-(arylmethyl)-ester group and leave the N-L-α-aspartyl-L-phenylalanine-1-lower alkyl ester product. n Novel intermediates for the synthesis 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:US-4656304-A
优先权日:1983-05-31
标 题 :Aspartame synthesis
发明人：OPPICI ERNESTO; DALLATOMASINA FRANCO; GIARDINO PIETRO
权利人:ERBA FARMITALIA
摘要:A process for the preparation of the N-L-α-aspartyl-L-phenylalanine 1-methyl ester (aspartame) which is characterized by adding phosphoric acid and a lower alkyl alcohol to the reaction mixture containing N-formyl α-L-aspartyl- and β-L-aspartyl-L-phenyl-alanine methyl ester and only one of the resultant deformylated isomers, i.e. aspartame phosphate precipitates. n The α-isomer phosphate is collected by filtration and converted to free aspartame by treatment with a base.

专利号:US-4549987-A
优先权日:1983-08-12
标题:Aspartame synthesis
发明人：DALLATOMASINA FRANCO; ORTICA ROBERTO; GIARDINO PIETRO; OPPICI ERNESTO
权利人:ERBA FARMITALIA
摘要:A process for deformylation and separation of N-formyl-L- α-aspartyl-L-phenylalanine methyl ester from a mixture containing both α and β isomers thereof, which comprises admixing with said isomeric mixture hydrogen peroxide and an organic acid.