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    Process for producing an addition compound of a dipeptide ester and an amino acid ester
    1.
    发明授权
    Process for producing an addition compound of a dipeptide ester and an amino acid ester 失效
    制备二肽酯和氨基酸酯的加成化合物的方法

    公开(公告)号：US4521514A

    公开(公告)日：1985-06-04

    申请号：US516344

    申请日：1983-07-22

    申请人： Kiyotaka Oyama ,  Shigeaki Irino ,  Tsuneo Harada ,  Masao Nakamura

    发明人： Kiyotaka Oyama ,  Shigeaki Irino ,  Tsuneo Harada ,  Masao Nakamura

    IPC分类号： C12P21/02 ,  C07K5/06 ,  C07K5/072 ,  C07K5/075 ,  C07C103/52

    CPC分类号： C07K5/0613

    摘要： A process for producing an addition compound of N-benzyloxycarbonyl-.alpha.-L-aspartyl-L-phenylalanine methyl ester and phenylalanine methyl ester. Benzyloxycarbonylation of the amino group of L-aspartic acid by benzyloxycarbonylchloride in the presence of a base and esterification of phenylalanine containing its L-body by methanol in the presence of an acid are carried out and both the reaction solutions are admixed after residual methanol is removed from the esterification reaction solution. A proteolytic enzyme is added to the resulting mixture solution after it is adjusted to have a pH, value, at which no substantial deactivation of the enzyme occurs. The reaction of N-benzyloxycarbonyl-L-aspartic acid and phenylalanine methyl ester is carried out in the solution at a pH, at which the proteolytic enzyme exerts the enzymatic activity to deposit the addition compound which is then recovered.

    摘要翻译： 制备N-苄氧羰基-α-L-天冬氨酰-L-苯丙氨酸甲酯和苯丙氨酸甲酯的加成化合物的方法。 苄基氧基羰基氯在碱存在下苄基氧基羰基化，苄基氧基羰基氯在碱的存在下苄基氧基羰基化，并在酸存在下用甲醇在酸的存在下酯化含有L-体的苯丙氨酸，并在残留的甲醇被除去后将两种反应溶液混合 从酯化反应溶液中。 在将所述混合溶液调节至具有不发生基本上的失活酶的pH值之后，将蛋白水解酶加入到所得混合溶液中。 N-苄氧羰基-L-天冬氨酸和苯丙氨酸甲酯的反应在溶液中在pH下进行，其中蛋白水解酶发挥酶活性以沉积加入的化合物，然后将其回收。

    Enzymatic coupling reaction of N-protected-L-aspartic acid and phenylalanine methyl ester
    2.
    发明授权
    Enzymatic coupling reaction of N-protected-L-aspartic acid and phenylalanine methyl ester 失效
    N-保护的L-天冬氨酸和苯丙氨酸甲酯的酶偶联反应

    公开(公告)号：US5693485A

    公开(公告)日：1997-12-02

    申请号：US729507

    申请日：1996-10-11

    申请人： Tsuneo Harada ,  Shigeaki Irino ,  Yukio Kunisawa ,  Kiyotaka Oyama

    发明人： Tsuneo Harada ,  Shigeaki Irino ,  Yukio Kunisawa ,  Kiyotaka Oyama

    IPC分类号： C12P13/04 ,  C07K5/072 ,  C12P21/02 ,  C12P21/00 ,  C07K5/06

    CPC分类号： C07K5/0613 ,  C12P21/02

    摘要： The invention relates to a process for the preparation of N-protected-L-aspartyl-L-phenylalanine methyl ester by enzymatic coupling of an N-protected-L-aspartic acid and L- or DL-phenylalanine methyl ester in an aqueous solution with formation of a precipitate using a thermolysin-like protease enzyme, wherein a water-immiscible organic solvent is added to and blended with the reaction system during the formation of the precipitate in the course of the coupling reaction, which organic solvent has a relatively high affinity for the precipitate. The process is particularly suitable as a continuous process. The method results in lower enzyme deactivation during and after the enzymatic coupling reaction and in larger and thicker precipitated crystals.

    摘要翻译： 本发明涉及通过N-保护的L-天冬氨酸和L-或DL-苯丙氨酸甲酯在水溶液中的酶偶联来制备N-保护的L-天冬氨酰基-L-苯丙氨酸甲酯的方法， 使用嗜热菌蛋白酶蛋白酶形成沉淀物，其中在偶联反应过程中在形成沉淀物期间向反应体系中加入与水不混溶的有机溶剂并与其混合，该有机溶剂具有较高的亲和力 为沉淀。 该方法特别适合作为连续方法。 该方法在酶偶联反应期间和之后以及较大和较厚的沉淀晶体中导致较低的酶失活。

    Process for producing alpha-aspartyl-l-phenylalanine methyl ester having an improved solubility
    5.
    发明授权
    Process for producing alpha-aspartyl-l-phenylalanine methyl ester having an improved solubility 失效
    生产具有改善的溶解度的α-天冬氨酰基-1-苯丙氨酸甲酯的方法

    公开(公告)号：US4810818A

    公开(公告)日：1989-03-07

    申请号：US78707

    申请日：1987-07-28

    申请人： Hidetoshi Wakamatsu ,  Shigeaki Irino ,  Tsuneo Harada ,  Akira Tokuda ,  Kiyotaka Oyama

    发明人： Hidetoshi Wakamatsu ,  Shigeaki Irino ,  Tsuneo Harada ,  Akira Tokuda ,  Kiyotaka Oyama

    IPC分类号： A23L27/30 ,  C07K1/00 ,  C07K5/072 ,  C07K5/075 ,  C07C101/02

    CPC分类号： C07K5/0613

    摘要： A process for producing dry .alpha.-L-aspartyl-L-phenylalanine methyl ester having an improved solubility from wet crystals of .alpha.-L-aspartyl-L-phenylalanine methyl ester having a water content of at least 20% by weight, which comprises drying the wet crystals at a temperature of higher than 50.degree. C. to obtain moist crystals having a water content of less than 20 and more than 15% by weight, then drying the moist crystals at a temperature of not higher than 50.degree. C. to obtain semi-dry crystals having a water content of less than 5% by weight, and further drying the semi-dry crystals at a temperature of higher than 50.degree. C. to obtain dry crystals of .alpha.-L-aspartyl-L-phenylalanine methyl ester.

    摘要翻译： 一种具有水含量为至少20重量％的α-L-天冬氨酰基-L-苯丙氨酸甲酯的湿结晶具有改善的溶解度的干燥α-L-天冬氨酰基-L-苯丙氨酸甲酯的方法，其包括干燥 在高于50℃的温度下的湿结晶，得到含水量小于20且大于15重量％的湿润结晶，然后在不高于50℃的温度下干燥湿结晶至 得到水分小于5重量％的半干燥晶体，并在高于50℃的温度下进一步干燥半干燥晶体，得到α-L-天冬氨酰基-L-苯丙氨酸甲酯的干结晶 酯。

    Process for recovering a dipeptide derivative
    7.
    发明授权
    Process for recovering a dipeptide derivative 失效
    回收二肽衍生物的方法

    公开(公告)号：US4487717A

    公开(公告)日：1984-12-11

    申请号：US415912

    申请日：1982-09-08

    申请人： Kiyotaka Oyama ,  Shigeaki Irino ,  Norio Hagi

    发明人： Kiyotaka Oyama ,  Shigeaki Irino ,  Norio Hagi

    IPC分类号： C07K5/072 ,  C07K5/075 ,  C07C103/52

    CPC分类号： C07K5/0613 ,  Y10S530/801

    摘要： A process for recovering a dipeptide derivative comprises admixing an aqueous mixture of a solid dipeptide ester derivative of the formula ##STR1## wherein R.sub.1 is a lower alkyl group, R.sub.2 is a side chain group of an amino acid, n is 1 or 2, X is a benzyloxycarbonyl group which can have a nuclear substituent and Y is a hydrogen ion or an ammonium derivative ion of the formula ##STR2## wherein R.sub.3 is a side chain group of an amino acid and R.sub.4 is a lower alkyl group with an organic solvent capable of forming a binary phase system with water; said solvent being present in an amount effective to obtain the transfer of said peptide in the form of a solid from the aqueous phase to the organic solvent phase, settling the resulting admixture to form(1) an organic solvent phase containing in a solid state a substantial amount of dipeptide derivative of the formula ##STR3## wherein R.sub.1, R.sub.2, n and X are as defined above and Z is a hydrogen ion or an ammonium derivative ion of the formula ##STR4## wherein R.sub.3 and R.sub.4 are as defined above, and (2) an aqueous phase, separating the organic solvent phase from the aqueous phase, and recovering the dipeptide derivative from the organic solvent phase.

    摘要翻译： 回收二肽衍生物的方法包括混合式（I）的固体二肽酯衍生物的水性混合物，其中R1是低级烷基，R2是氨基酸的侧链基团，n是1或 2，X是可以具有核取代基的苄氧基羰基，Y是氢离子或式（II）的铵衍生物离子，其中R3是氨基酸的侧链基团，R4是低级烷基 与能够与水形成二元相体系的有机溶剂组合; 所述溶剂的存在量有效地获得将固体形式的所述肽从水相转移到有机溶剂相，沉淀所得混合物以形成（1）含有固态的有机溶剂相a （III）的大量二肽衍生物，其中R 1，R 2，n和X如上所定义，Z是下式的氢离子或铵衍生物离子，其中R 3和R 4 如上所定义，和（2）水相，将有机溶剂相与水相分离，并从有机溶剂相中回收二肽衍生物。

    Method for producing optically active amino acid of derivative thereof having high optical purity
    9.
    发明授权
    Method for producing optically active amino acid of derivative thereof having high optical purity 失效
    光学纯度高的光学活性氨基酸或其衍生物的制造方法

    公开(公告)号：US6008403A

    公开(公告)日：1999-12-28

    申请号：US938670

    申请日：1997-09-26

    申请人： Kimio Katsuura ,  Shigeaki Irino ,  Akira Tokuda

    发明人： Kimio Katsuura ,  Shigeaki Irino ,  Akira Tokuda

    IPC分类号： C07C227/34 ,  C07C227/40 ,  C07C227/42 ,  C07C229/36 ,  C07C229/00 ,  C07B57/00

    CPC分类号： C07C227/34 ,  C07C227/40 ,  C07C227/42 ,  C07B2200/07

    摘要： A method for producing an optically active amino acid or derivative thereof having a high optical purity from an optically active amino acid comprising optical isomers or derivative thereof, which comprises any one of processes (A), (B), and (C), wherein the process (A) comprises the steps: (1) previously preparing an optically active amino acid or derivative thereof having an optical purity higher than a convergent value of a mutual solubility of the optical isomers and (2) crystallizing the optically active amino acid or the derivative thereof that exists in excess, said convergent value being a ratio of the desired optical isomer in the optical isomers dissolved in a mother liquor in which crystals of a racemate and an optically active compound coexist at equilibrium (the optical purity in a mother liquor). The processes (B) and (C) are described in the specification.

    摘要翻译： 包含光学异构体或其衍生物的光学活性氨基酸具有高光学纯度的光学活性氨基酸或其衍生物的方法，其包括方法（A），（B）和（C）中的任一种，其中 方法（A）包括以下步骤：（1）预先制备光学纯度高于光学异构体相互溶解度的收敛值的光学活性氨基酸或其衍生物，和（2）使光学活性氨基酸结晶或 所述收敛值是溶解在母液中的旋光异构体中所需的旋光异构体的比例，其中外消旋体和光学活性化合物的晶体在平衡时共存（母液中的光学纯度 ）。 方法（B）和（C）在说明书中描述。