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    Process for producing .alpha.-L-aspartyl-L-phenylalanine methyl ester for its hydrochloride
    3.
    发明授权
    Process for producing .alpha.-L-aspartyl-L-phenylalanine methyl ester for its hydrochloride 失效
    制备α-L-天冬氨酰-L-苯丙氨酸甲酯为其盐酸盐的方法

    公开(公告)号：US4684745A

    公开(公告)日：1987-08-04

    申请号：US484506

    申请日：1983-04-13

    申请人： Tadashi Takemoto ,  Yasuo Ariyoshi

    发明人： Tadashi Takemoto ,  Yasuo Ariyoshi

    IPC分类号： C07C231/00 ,  C07C67/00 ,  C07C231/12 ,  C07K5/075 ,  C07C101/32

    CPC分类号： C07K5/0613

    摘要： A process for producing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrochloride which comprises contacting N-formyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester with a mixture of methanol and a highly concentrated hydrochloric acid at a temperature of between 0.degree. and 40.degree. C., whereby the amino-protecting formyl group is removed and .alpha.-L-aspartyl-L-phenylalanine methyl ester crystalizes, and isolating the hydrochloride crystals, and, if desired, converting the hydrochloride to free .alpha.-L-aspartyl-L-phenylalanine methyl ester, is disclosed along with variations thereof. The process is commerically advantageous in that it utilizes inexpensive materials while minimizing hydrolysis of the peptide bond.

    摘要翻译： 制备α-L-天冬氨酰-L-苯丙氨酸甲酯或其盐酸盐的方法，其包括使N-甲酰基-α-天冬氨酰基-L-苯丙氨酸甲酯与甲醇和高浓度盐酸的混合物在温度 在0至40℃之间，由此除去氨基保护甲酰基，α-L-天冬氨酰基-L-苯丙氨酸甲酯结晶，并分离盐酸盐晶体，如果需要，将盐酸转化为游离α -L-天冬氨酰基-L-苯丙氨酸甲酯及其变体。 该方法在商业上是有利的，因为它使用便宜的材料，同时使肽键的水解最小化。

    Formation of peptide bonds in the presence of isonitriles
    4.
    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
    5.
    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。