首页> 外国专利> Process for the preparation of compound Intermediate N - acetyl - (L) - 4 - (L) - cianofenilalanina AC PHE (CN) - Oh is particularly useful in the preparation of N - acetyl - (L) - P - amidinofenilalanina - ciclohexIlglicina beta - (3) - N - metilpiridinio) alanine and Procedure for the preparation of compound N - acetyl - (L) - P - ciclohexilglicina amidinofenilalanina - beta - (3) - N - metilpiridinio) alanine

Process for the preparation of compound Intermediate N - acetyl - (L) - 4 - (L) - cianofenilalanina AC PHE (CN) - Oh is particularly useful in the preparation of N - acetyl - (L) - P - amidinofenilalanina - ciclohexIlglicina beta - (3) - N - metilpiridinio) alanine and Procedure for the preparation of compound N - acetyl - (L) - P - ciclohexilglicina amidinofenilalanina - beta - (3) - N - metilpiridinio) alanine

机译:制备化合物中间体N-乙酰基-(L)-4-(L)-钢琴芬拉拉尼娜AC PHE(CN)-OH在制备N-乙酰基-(L)-P-酰胺基菲拉拉尼娜-ciclohexIlglicina beta中特别有用-(3)-N-甲丙啶化丙氨酸和制备化合物N-乙酰基-(L)-P-环己基丙氨酸-β-(3)-N-甲丙啶化丙氨酸的制备方法

摘要

The present Invention relates to a process for the preparation of N - acetyl - (L) - 4 - cianofenilalanina from Racemic Ester Compound etilicode N - acetyl - (D,L) - cianofenilalanina understand the stages of combining this compuestoracemi co, a sufficient amount of an aqueous solution, sufficient amount of acetonitrileA sufficient amount of subtilisin to react with a substantial amount of Racemic Compound formarun reaction medium to adjust the Med's reaction when an appropriate pHAde subtilisin and maintenance of proper pH while unareaccion takes place to produce the desired Compound.Also described is a method for obtaining N - acetyl - (L) - amido phenylalanine ciclohexilglicina beta - (3) - N - metilpiridinio) alanine, which comprises the steps of the intermediary - copulate ACETIl - (L) - 4 - cianofenilalanina with amide (L) - ciclohexilglicina - (L) - beta - (3-pyridyl) - alanine yconversion, cyano Group of this Compound copulated,In the Group amidino and methylation delpiridilo nitrogen to give the desired Compound is particularly useful in the inhibition of factor Xa in the clotting of Blood.
机译:本发明涉及一种由消旋酯化合物etilicode制备N-乙酰基-(L)-4-钢琴粉的方法。N-乙酰基-(D,L)-钢琴粉基的理解充分结合该compuestoracemi co的步骤。水溶液,足够量的乙腈,足够量的枯草杆菌蛋白酶,可与大量消旋化合物formarun反应介质反应,以调节适当的pHAde枯草杆菌蛋白酶时的Med反应,并维持适当的pH值,而不会产生不期望的化合物。还描述了一种获得N-乙酰基-(L)-酰胺基苯基丙氨酸环己基丙氨酸β-(3)-N-甲吡哌啶酮)丙氨酸的方法,该方法包括以下步骤:-交联ACETIl-(L)-4-具有酰胺的氰基芬尼拉兰纳。 (L)-环己基硅氧烷-(L)-β-(3-吡啶基)-丙氨酸转化,该化合物的氰基交联,在mid基和甲基化delpiridilon中产生所需化合物的雌激素在凝血中抑制因子Xa特别有用。

著录项

  • 公开/公告号AR005119A1

    专利类型

  • 公开/公告日1999-04-14

    原文格式PDF

  • 申请/专利权人 AVENTIS PHARMACEUTICALS INC.;

    申请/专利号AR1996P105740

  • 发明设计人

    申请日1996-12-18

  • 分类号C12P13/04;C12P13/22;C07C231/12;C07C255/60;C07D213/40;C07K5/06;C07K5/08;C07K5/09;C12P13/02;C12P21/02;C12P41;

  • 国家 AR

  • 入库时间 2022-08-22 02:28:28

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