CAS: 3479-47-8; Z-Asp(Obzl)-Oh

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5241-62-3 2177-63-1 51186-58-4

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📜对甲苯磺酸置于1,4-二氧六环,Sodium Hydroxide,甲苯体系中,化学反应生成 Cbz-L-天门冬氨酸β-苄酯
参考文献:Poly-L-Aspartic Acid
标题:Poly-L-Aspartic Acid
摘要:
DOI:10.1021/ja01153A009

专利信息

专利号:EP-0463070-B1
优先权日:1989-03-14
标 题 :A process for producing pentapeptides and intermediates for use in the synthesis
摘要:Pentapeptides having the formula H-Asp-Ser-C-Pro-Arg-OH, where Asp, Ser, Pro and Arg may have L- or D-configuration, and C denotes Asp or Asn in L or D configuration, are synthesized by reacting in an aqueous medium Y2-Pro-OH, wherein Y2 is a protective group, with Arg-Ro, wherein Ro is OH or is as defined below for R1 below, to form Y2-Pro-Arg-Ro, which is deprotected, if necessary under conversion to Pro-Arg-R1, wherein R1 is an enzymatically cleavable alpha -carboxy substituting group selected from esters, amides, anilides, hydrazides or L-amino acid esters, and thereafter reacting Y3-C(Z3)-OH with Pro-Arg-R1 to form Y3-C(Z3)-Pro-Arg-R1, which is deprotected to C-Pro-Arg-R1, and then reacting Y4-Ser-OH with C-Pro-Arg-R1 to form Y4-Ser-C-Pro-Arg-R1, which is deprotected to Ser-C-Pro-Arg-R1, and reacting Y5-Asp(Z5)-OH with Ser-C-Pro-Arg-R1 to form Y5-Asp(Z5)-Ser-C-Pro-Arg-R1, which is deprotected to the intermediate Asp-Ser-C-Pro-Arg-R1, and finally removing the group R1 with an enzyme, preferably trypsin to form Asp-Ser-C-Pro-Arg, or removing R1 from Y5-Asp(Z5)-Ser-C-Pro-Arg-R1 before deprotection to Asp-Ser-C-Pro-Arg-OH. The groups Y2, Y3, Y4, Y5, Z3 and Z5 are protective groups which apart from Y2 are removable by catalytic hydrogenation. The employed synthesis strategy based on the combination hydrogenation/enzyme, both proceeding under mild conditions, leads to the peptides, in particular HEPP, in good yield without risk of formation of beta -aspartyl peptides and cleavage of Asp-Pro bonds.

专利号:US-3933783-A
优先权日:1971-12-27
标 题 :Formation of peptide bonds in the presence of isonitriles
发明人：YASUDA NAOHIKO; ARIYOSHI YASUO; TOI KOJI
权利人:AJINOMOTO KK
摘要:Amino acids having masked amino groups react with amino acids having masked carboxyl groups to form peptide derivatives in good yields if the reaction medium contains an isonitrile. Isonitriles also are effective in causing condensation of amino acids having masked amino groups with compounds having active hydroxyl groups to the corresponding amino acid esters. The yields of the first-mentioned reaction are enhanced if the reaction mixture additionally contains one of the compounds having active hydroxyl groups. Both the peptide derivatives and the amino acid esters of the compounds having active hydroxyl groups are useful for peptide synthesis.

专利号:US-3984417-A
优先权日:1971-12-27
标题:Method of producing active amino acid esters
发明人：YASUDA NAOHIKO; ARIYOSHI YASUO; TOI KOJI
权利人:AJINOMOTO KK
摘要:Amino acids having masked amino groups react with amino acids having masked carboxyl groups to form peptide derivatives in good yields if the reaction medium contains an isonitrile. Isonitriles also are effective in causing condensation of amino acids having masked amino groups with compounds having active hydroxyl groups to the corresponding amino acid esters. The yields of the first-mentioned reaction are enhanced if the reaction mixture additionally contains one of the compounds having active hydroxyl groups. Both the peptide derivatives and the amino acid esters of the compounds having active hydroxyl groups are useful for peptide synthesis.

专利号:BE-898650-A
优先权日:1983-01-13
标题:SYNTHESIS OF ASPARTAME

专利号:DE-3400746-A1
优先权日:1983-01-13
标 题 :METHOD FOR THE SYNTHESIS OF ASPARTAM

专利号:EP-0135429-A1
优先权日:1983-08-16
标 题 :The synthesis of cyclopropane amino acids and peptides