Process for the preparation of
6-demethyl-6-deoxy-6-methylene-5-oxytetracyclin and the
11A-chloro-derivative thereof
    3.
    发明授权
    Process for the preparation of 6-demethyl-6-deoxy-6-methylene-5-oxytetracyclin and the 11A-chloro-derivative thereof 失效
    6-脱甲基-6-脱氧-6-亚甲基-5-氧四环素及其11A-氯衍生物的制备方法

    公开(公告)号:US4659515A

    公开(公告)日:1987-04-21

    申请号:US646574

    申请日:1984-08-31

    摘要: The invention relates to a new and improved process for the preparation of 6-demethyl-6-deoxy-6-methylene-5-oxytetracycline and the 11a-chloro derivative thereof by dehydrating 11a-chloro-5-oxytetracycline-6,12-hemiketal, which comprises treating 11a-chloro-5-oxytetracycline-6,12-hemiketal or an acid salt thereof with a dehydrating mixture formed by the reaction of chloro sulfonic acid and formic acid and isolating the 11a-chloro-6-demethyl-6-deoxy-6-methylene-5-oxytetracycline and salt thus obtained and optionally dehalogenating the same by reaction with a reducing agent.The advantage of the process of the present invention is that it is simple, economical and suitable for industrial scale manufacture and provides a pure product of high quality by excellent yields.

    摘要翻译: 本发明涉及一种通过使11a-氯-5-氧四环素-6,12-半缩酮脱水制备6-脱甲基-6-脱氧-6-亚甲基-5-土霉素及其11a-氯衍生物的新方法和改进方法 其包括用与氯磺酸和甲酸的反应形成的脱水混合物处理11a-氯-5-土霉素-6,12-半缩酮或其酸盐,并将11a-氯-6-去甲基-6- 脱氧-6-亚甲基-5-土霉素和盐,并通过与还原剂反应任选地使其脱卤。 本发明方法的优点在于它简单,经济,适用于工业规模的制造,并通过优异的成品率提供高品质的纯净产品。

    Process for the preparation of benzimidazole-thiol
    4.
    发明授权
    Process for the preparation of benzimidazole-thiol 失效
    苯并咪唑硫醇的制备方法

    公开(公告)号:US4675413A

    公开(公告)日:1987-06-23

    申请号:US811246

    申请日:1985-12-19

    IPC分类号: C07D235/32 C07D235/04

    CPC分类号: C07D235/32

    摘要: A new process is disclosed for preparing a compound of the formula (I) ##STR1## wherein R is C.sub.1 to C.sub.5 alkyl; which comprises reducing a compound of the formula (II) ##STR2## or salt thereof wherein A is --SO.sub.2 X, --SOH, --SOA.sup.1, or --SA.sup.1 group,X is chlorine or hydrogen; andA.sup.1 is a group of the Formula ##STR3## with the aid of aluminum activated with a catalytic amount of a metal and/or metal salt in a mixture of water, a mineral acid, and an aliphatic carboxylic acid having 1 to 3 carbon atoms at a temperature of 0.degree. to 100.degree. C., thereafter, optionally, the product is recovered from an acid medium at a pH range of 2 to 3 in crystalline form.

    摘要翻译: 公开了用于制备式(I)化合物的新方法,其中R是C1至C5烷基; 其包括还原式(II)的化合物或其盐,其中A是-SO 2 X,-SOH,-SOA 1或-SA 1基团,X是氯或氢; 并且A1是通过在水,无机酸和具有1至3个碳原子的脂族羧酸的混合物中催化量的金属和/或金属盐活化的铝的助催化剂的组合的“IMAGE” 在0℃至100℃的温度下,然后,任选地,该产物从酸性介质中以2至3的结晶形式从pH值范围内回收。