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    Process for the enzymatic preparation of protected and unprotected di- and oligopeptides in aqueous solutions
    1.
    发明授权
    Process for the enzymatic preparation of protected and unprotected di- and oligopeptides in aqueous solutions 失效
    在水溶液中酶法制备受保护和未保护的二肽和寡肽的方法

    公开(公告)号：US5304470A

    公开(公告)日：1994-04-19

    申请号：US823956

    申请日：1992-01-23

    申请人： Andreas Fischer ,  Alexander Schwarz ,  Christian Wandrey ,  Guenter Knaup ,  Andreas Bommarius ,  Karl-Heinz Drauz

    发明人： Andreas Fischer ,  Alexander Schwarz ,  Christian Wandrey ,  Guenter Knaup ,  Andreas Bommarius ,  Karl-Heinz Drauz

    IPC分类号： C07C229/12 ,  C07K1/00 ,  C07K5/06 ,  C12P21/00 ,  C12P21/02 ,  C07K1/06 ,  C07K1/14

    CPC分类号： C12P21/02

    摘要： Protected and unprotected di- or oligopeptides are synthesized by reacting an N-terminally protected .alpha.-amino acid alkyl ester or peptide alkyl ester of the formula X--E--R.sup.1 with an amino acid or a di- or oligopeptide or a derivative thereof of the formula H.sub.2 N--Q--R.sup.2 in aqueous solution in the presence of a hydrolase, and, removing protective groups from the reaction product separated from the reaction mixture, where E is the residue of an .alpha.-amino acid or of a di- or oligopeptide, R.sup.1 is lower alkyl and X is a group which carries a charge or is polar at the pH values used for the reaction and which increases the solubility by a factor >5 compared with compounds wherein X=H, Q is the residue of an amino acid or of a di- or oligopeptide, and R.sup.2 is an optionally esterified or amidated acid group. In a preferred embodiment, the peptide or (.alpha.-)amino acid ester concentration is greater than 50 mM, wherein in a particularly preferred embodiment, the concentration ranges from 100 to 1000 mM with approximately comparable nucleophile and electrophile concentrations. The preferred substrate/enzyme ratios are >10.sup.5 M/M or >10.sup.3 M/M when papain is employed. Phthalyl, maleyl or citraconyl radicals and their derivatives or N-betainyl compounds are envisaged for use radicals (X) in the electrophilic component.

    摘要翻译： 受保护和未保护的二肽或寡肽通过使N-末端保护的（α） - 氨基酸烷基酯或式XE-R1的肽烷基酯与氨基酸或二肽或其寡肽或其衍生物 在水溶液存在下，在水溶液中制备式H2N-Q-R2，并且从反应混合物中分离出的反应产物中除去保护基团，其中E是（α） - 氨基酸或二 寡肽，R1是低级烷基，X是在用于反应的pH值下带有电荷或极性的基团，并且与其中X = H的化合物相比，其溶解度增加> 5倍，Q是 氨基酸或二肽或寡肽，R2是任选酯化或酰胺化的酸基团。 在优选的实施方案中，肽或（（α） - ）氨基酸酯浓度大于50mM，其中在特别优选的实施方案中，浓度范围为100至1000mM，具有大致相似的亲核试剂和亲电试剂浓度。 当使用木瓜蛋白酶时，优选的底物/酶比率> 105M / M或> 103M / M。 假定邻苯二甲酰基，马来酰基或柠康酰基及其衍生物或N-甜菜碱化合物在亲电子组分中使用基团（X）。