Process for producing 4-(2-methoxyethyl)-phenyl-glycidyl ether and/or
metoprolol
    3.
    发明授权
    Process for producing 4-(2-methoxyethyl)-phenyl-glycidyl ether and/or metoprolol 失效
    制备4-(2-甲氧基乙基) - 苯基 - 缩水甘油醚和/或美托洛尔的方法

    公开(公告)号:US4956284A

    公开(公告)日:1990-09-11

    申请号:US826791

    申请日:1986-02-06

    摘要: A process for the preparation of metoprolol in a stereospecific form or a non-toxic, pharmaceutically acceptable acid addition salt thereof and/or a stereospecific form of 4-(2-methoxyethyl)-phenyl glycidyl ether which comprises subjecting 4-(2-methoxyethyl)-phenyl allyl ether to the action of a microorganism having the ability for stereoselective epoxidation of 4-(2-methoxyethyl)-phenyl allyl ether into 4-(2-methoxyethyl)-phenyl glycidyl ether having at least 80% by weight the S configuration, at least partly separating 4-(2-methoxyethyl)-phenyl glycidyl ether and/or reacting 4-(2-methoxyethyl)-phenyl glycidyl ether with isopropylamine and at least partly separating metoprolol and/or converting metoprolol into its non-toxic, pharmaceutically acceptable acid addition salt.

    摘要翻译: 以立体特异性形式或无毒的药学上可接受的酸加成盐和/或立体特异性形式的4-(2-甲氧基乙基) - 苯基缩水甘油醚制备美托洛尔的方法,其包括使4-(2-甲氧基乙基) (4-甲氧基乙基) - 苯基烯丙基醚的4-(2-甲氧基乙基) - 苯基缩水甘油醚的立体选择性环氧化反应能力的微生物的作用,其具有至少80重量%的S 至少部分分离4-(2-甲氧基乙基) - 苯基缩水甘油醚和/或使4-(2-甲氧基乙基) - 苯基缩水甘油醚与异丙胺反应,并至少部分分离美托洛尔和/或将美托洛尔转化为无毒的 ,药学上可接受的酸加成盐。

    Process for the preparation of R-2,2-R.sub.1,R.sub.2
-1,3-dioxolane-4-methanol
    4.
    发明授权
    Process for the preparation of R-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol 失效
    制备R-2,2-R1,R2-1,3-二氧戊环-4-甲醇的方法

    公开(公告)号:US5190867A

    公开(公告)日:1993-03-02

    申请号:US822653

    申请日:1992-01-21

    摘要: Process for the preparation of R-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol wherein R.sub.1 and R.sub.2 are H or alkyl groups or wherein R.sub.1 and R.sub.2 together with the carbon atom to which they are attached form a carbocyclic ring by subjecting a mixture of R- and S-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol to the action of a micro-organism or substances derived therefrom having the ability for stereoselective consumption of S-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol preferably until at least 80 wt % and more preferably all the S-2,2-R.sub.1,R.sub.2 -1,3-dioxolane-4-methanol is consumed. Various micro-organisms of the genus Rhodococcus, Nocardia and Corynebacterium are disclosed as suitable for the purpose. The R-isomer is a valuable intermediate for stereospecific synthesis of various biologically active compounds including S-metoprolol.

    摘要翻译: 制备R-2,2-R1,R2-1,3-二氧戊环-4-甲醇的方法,其中R 1和R 2为H或烷基或其中R 1和R 2与它们所连接的碳原子一起形成 通过使R-和S-2,2-R1,R2-1,3-二氧戊环-4-甲醇的混合物经受微生物或其衍生物质的作用,具有立体选择性消耗S- 优选直到至少80重量%,更优选全部S-2,2-R 1,R 2,1,3-二氧戊环-4-甲醇被消耗 。 公开了红球菌属,诺卡氏菌属和棒状杆菌属的各种微生物,以适合此目的。 R-异构体是用于立体特异性合成各种生物活性化合物(包括S-美托洛尔)的有价值的中间体。