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    Process for producing an .alpha.-L-aspartyl-L-phenylalanine lower alkyl ester
    1.
    发明授权
    Process for producing an .alpha.-L-aspartyl-L-phenylalanine lower alkyl ester 失效
    制备α-L-天冬氨酰基-L-苯丙氨酸低级烷基酯的方法

    公开(公告)号：US4332718A

    公开(公告)日：1982-06-01

    申请号：US126671

    申请日：1980-03-04

    申请人： Satoji Takahashi ,  Koji Toi

    发明人： Satoji Takahashi ,  Koji Toi

    IPC分类号： A23L27/30 ,  C07C231/02 ,  C07D307/66 ,  C07K5/075 ,  C07C103/52 ,  C07D307/60

    CPC分类号： C07K5/0613 ,  C07D307/66 ,  Y10S530/801

    摘要： A process for producing an .alpha.-L-aspartyl-L-phenylalanine lower alkyl ester or its hydrochloride which comprises (a) treating an L-N-(1-methyl-2-lower aliphatic acylvinyl or 1-methyl-2-lower alkoxycarbonylvinyl)-aspartic acid or an alkali metal salt thereof with a dehydrating agent in an organic solvent containing an acid, (b) reacting the solution resulting from such treatment with an L-phenylalanine lower alkyl ester and (c) treating the resulting reaction mixture with water or an aqueous acid solution to remove the 1-methyl-2-lower aliphatic acylvinyl or 1-methyl-2-lower alkoxycarbonylvinyl group from the L-N-(1-methyl-2-lower aliphatic acylvinyl or 1-methyl-2-lower alkoxycarbonylvinyl)-aspartyl-L-phenylalanine lower alkyl ester is disclosed, along with L-N-(1-methyl-2-acetylvinyl)-aspartic acid anhydride.

    摘要翻译： 一种制备α-L-天冬氨酰基-L-苯丙氨酸低级烷基酯或其盐酸盐的方法，其包括（a）将LN-（1-甲基-2-低级脂族酰基乙烯基或1-甲基-2-低级烷氧基羰基乙烯基） - 天冬氨酸或其碱金属盐与脱水剂在含有酸的有机溶剂中反应，（b）使由此处理得到的溶液与L-苯丙氨酸低级烷基酯反应，和（c）用水或 从LN-（1-甲基-2-低级脂族酰基乙烯基或1-甲基-2-低级烷氧基羰基乙烯基）中除去1-甲基-2-低级脂肪族酰基乙烯基或1-甲基-2-低级烷氧基羰基乙烯基的酸水溶液， 公开了天冬氨酰-L-苯丙氨酸低级烷基酯以及LN-（1-甲基-2-乙酰基乙烯基） - 天冬氨酸酐。

    Formation of peptide bonds in the presence of isonitriles
    5.
    发明授权
    Formation of peptide bonds in the presence of isonitriles 失效
    在存在亚硝酸盐的情况下形成肽键

    公开(公告)号：US3933783A

    公开(公告)日：1976-01-20

    申请号：US530494

    申请日：1974-12-09

    申请人： Naohiko Yasuda ,  Yasuo Ariyoshi ,  Koji Toi

    发明人： Naohiko Yasuda ,  Yasuo Ariyoshi ,  Koji Toi

    IPC分类号： C07K1/10 ,  C07C103/52

    CPC分类号： C07C251/00 ,  C07K1/10

    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.

    摘要翻译： 如果反应介质含有异腈，具有掩蔽的氨基的氨基酸与具有掩蔽的羧基的氨基酸反应以以良好的产率形成肽衍生物。 异腈还有效地使具有掩蔽氨基的氨基酸与具有活性羟基的化合物缩合成相应的氨基酸酯。 如果反应混合物另外含有具有活性羟基的化合物之一，则提高反应​​的产率。 肽衍生物和具有活性羟基的化合物的氨基酸酯都可用于肽合成。

    Method of producing active amino acid esters
    7.
    发明授权
    Method of producing active amino acid esters 失效
    生产活性氨基酸酯的方法

    公开(公告)号：US3984417A

    公开(公告)日：1976-10-05

    申请号：US530495

    申请日：1974-12-09

    申请人： Naohiko Yasuda ,  Yasuo Ariyoshi ,  Koji Toi

    发明人： Naohiko Yasuda ,  Yasuo Ariyoshi ,  Koji Toi

    IPC分类号： A61K38/00 ,  C07D215/26 ,  C07K1/06 ,  C07K1/08 ,  C07K1/10 ,  C07D215/24 ,  C07C101/19 ,  C07C103/52

    CPC分类号： C07C251/00 ,  C07K1/064 ,  C07K1/084 ,  C07K1/10 ,  A61K38/00

    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.

    摘要翻译： 如果反应介质含有异腈，具有掩蔽的氨基的氨基酸与具有掩蔽的羧基的氨基酸反应以以良好的产率形成肽衍生物。 异腈还有效地使具有掩蔽氨基的氨基酸与具有活性羟基的化合物缩合成相应的氨基酸酯。 如果反应混合物另外含有具有活性羟基的化合物之一，则提高反应​​的产率。 肽衍生物和具有活性羟基的化合物的氨基酸酯都可用于肽合成。