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发明公开
CN101628899A 1-(2-甲氧基苯基)-4-[3-(萘-1-氧基)-2-羟基丙基]哌嗪光学异构体及其盐、制备方法和应用 无效 - 撤回

1-(2-甲氧基苯基)-4-[3-(萘-1-氧基)-2-羟基丙基]哌嗪光学异构体及其盐、制备方法和应用
摘要：
本发明涉及由以下式(1)或式(2)表示的1-(2-甲氧基苯基)-4-[3-(萘-1-氧基)-2-羟基丙基]哌嗪的光学异构体R或S，还涉及它们的制备方法，其特征是用R-或S-对甲苯磺酰缩水甘油酯与1-萘酚反应生成的中间体与1-(2-甲氧苯基)哌嗪反应得到，或者用消旋环氧氯丙烷与1-萘酚反应生成的中间体与1-(2-甲氧苯基)哌嗪反应得到。另外还涉及该光学异构体R或S的应用和其所有生理上可接受的无机盐类或有机盐类。由于该光学异构体R和S为选择性α 1 肾上腺素受体拮抗剂，对前列腺增生和高血压有明显抑制作用，且比目前临床上使用的α 1 受体阻断剂具有更高的选择性和更小的毒副作用，因此可用于制备治疗前列腺增生和高血压的药物。
摘要（英）：

The invention relates to an optical isomer R or S of 1-(2-methoxypheny1)-4-[3-(naphthalene-1-oxy)-2-hydroxypropyl] piperazine expressed by the following formula (1) or formula (2), and also relates to a preparation method thereof. The optical isomer is characterized in that the optical isomer is obtained by the reaction of 1-(2-methoxypheny1) piperazine and intermediate which is generated by the reaction of R- or S-p-toluenesulfonyl glycidyl ester and 1-naphthol, or obtained by the reaction of 1-(2-methoxypheny1) piperazine and intermediate which is generated by the reaction of racemic epoxy chloropropane and 1-naphthol. In addition, the invention also relates to application of the optical isomer R or S and physiologically acceptable inorganic salt or organic salt thereof. Because the optical isomer R and S are selective alpha1 epinephrine receptor antagonists which have obvious inhibiting effects on benign prostatic hyperplasia and hypertension and have higher selectivity and less toxic and side effects compared with the prior alpha1 receptor antagonists used in clinic, the optical isomer R and S can be used for preparing medicaments for treating the benign prostatic hyperplasia and the hypertension.

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