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1. 发明授权

US5290958A Phase transfer catalytic process for preparing intermediates of atenolol, propranolol, and their derivatives 失效
标题翻译：用于制备阿替洛尔，普萘洛尔及其衍生物的中间体的相转移催化方法
公开(公告)号：US5290958A
公开(公告)日：1994-03-01
申请号：US33047
申请日：1993-08-18
申请人： Shyue-Ming Jang , Tian-Shy Shieh
发明人： Shyue-Ming Jang , Tian-Shy Shieh
IPC分类号： C07C41/16 , C07D301/28 , C07D303/22 , C07C41/03 , C07C43/205 , C07D303/23
CPC分类号： C07D303/22 , C07C41/16
摘要： A phase transfer catalytic process for the preparation of epoxide and halohydrin intermediates, which can be subsequently and directly reacted with isopropylamine to produce beta-adrenergic antagonists such as atenolol, propanolol and their derivatives. In the process disclosed in the present invention, quaternary ammonium salts of high alkyl groups or tertiary ammonium salts of lower alkyl groups are used as catalyst in the phase transfer catalytic oxygenated-alkylation reaction between an aromatic alcohol such as p-hydroxyphenyl acetamide (for the production of atenolol) or .alpha.-naphthol (for the production of propranolol) and epichlorohydrin to yield epoxide and halohydrin intermediates. The quaternary ammonium salts of high alkyl groups are represented by the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are C.sub.1 to C.sub.20 alkyl groups and at least one of the R.sub.1, R.sub.2, R.sub.3, or R.sub.4 is a C.sub.9 to C.sub.20 alkyl group, and X is a halide group. And the tertiary ammonium salts of lower alkyl groups are presented by the following formula: ##STR2## wherein R.sub.5 is a C.sub.1 to C.sub.20 alkyl group, H is hydrogen, and X is a halide group.
摘要翻译：用于制备环氧化物和卤代醇中间体的相转移催化方法，其可以随后和异丙胺直接反应以产生β-肾上腺素能拮抗剂，例如阿替洛尔，丙酰洛伦及其衍生物。在本发明公开的方法中，在芳基醇如对羟基苯基乙酰胺之间的相转移催化氧化 - 烷基化反应中使用高级烷基的季铵盐或低级烷基的叔铵盐作为催化剂（对于产生阿替洛尔）或（α） - 萘酚（用于生产普萘洛尔）和表氯醇以产生环氧化物和卤代醇中间体。高烷基的季铵盐由下式表示：（*化学结构*）其中R 1，R 2，R 3和R 4是C 1至C 20烷基和R 1，R 2，R 3或R 4中的至少一个是C 9〜20烷基，X是卤化物基团。低级烷基的叔铵盐由下式表示：（*化学结构*）其中R 5为C 1至C 20烷基，H为氢，X为卤化物基团。

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