首页> 外国专利> approach to the use of racemic amp; alpha; - hydroxy - amp; beta;, amp; beta; dimethyl amp; gamma; - butyrolactone in the optically active and their counterparts.

approach to the use of racemic amp; alpha; - hydroxy - amp; beta;, amp; beta; dimethyl amp; gamma; - butyrolactone in the optically active and their counterparts.

机译:外消旋和α的使用方法; -羟基-&beta ;,β二甲基和γ; -光学活性中的丁内酯及其对应物。

摘要

A process for resolving D,L-pantolactone uses as the resolving agent a 1,4a -dimethyl-7-isopropyl-octahydro-, dodecahydro-, or per-hydrophenanthrene derivative which is substituted at the 1-position with a -NH2 or -CH2NH2 group. The salts of a ,q -dihydroxy-b b -dimethyl butyric acid with the above bases, formed during the resolution, are claimed per se. Preferably, the sodium salt of a racemic mixture of this acid is first formed from the pantolactone and is reacted with 55 to 57 molar per cent of the phenanthrene derivative hydrochloride. At equilibrium the L-( - )-salt of the phenanthrene derivative precipitates. Thus D-( - )-pantolactone may be formed from the D-( + )-sodium salt left in solution by acidification, and L-( + )-pantolactone may be formed via its sodium salt, and then racemized to form fresh starting material. Exemplified amines of the above formula used for the resolution are the D 5, D 7, D 46-8a octahydro, D 8 dodecahydro and perhydro derivatives.
机译:解决D,L-泛内酯的方法使用1,4a-二甲基-7-异丙基-八氢-,十二氢-或全氢菲衍生物作为拆分剂,该衍生物在1-位被-NH 2或-取代。 CH 2 NH 2基团。本身要求保护在分解过程中形成的,q-二羟基-b b-二甲基丁酸与上述碱的盐。优选地,该酸的外消旋混合物的钠盐首先由泛内酯形成,并与55-57摩尔%的菲衍生物盐酸盐反应。在平衡时,菲衍生物的L-(-)盐沉淀。因此,可以通过酸化由溶液中残留的D-(+)-钠盐形成D-(-)-泛内酯,然后可以通过其钠盐形成L-(+)-泛内酯,然后消旋形成新的起始原料。材料。用于拆分的上式的示例性胺为D 5,D 7,D 46-8a八氢,D 8十二氢和全氢衍生物。

著录项

  • 公开/公告号DK116726B

    专利类型

  • 公开/公告日1970-02-09

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE & CO.;

    申请/专利号DK19660002078

  • 发明设计人 F HOFFMANN LA ROCHE CO AG;

    申请日1966-04-22

  • 分类号C07D5/06;

  • 国家 DK

  • 入库时间 2022-08-23 11:35:46

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