1-苯磺酰基哌嗪 、 环氧氯丙烷 以to give 1.7 g of 1-benzenesulfonyl-4-(3-chloro-2-hydroxypropyl)piperazine as a colorless powdery crystal的产率得到1-benzenesulfonyl-4-(3-chloro-2-hydroxypropyl)piperazine
A propane derivative represented by the following formula
wherein R represents a lower alkyl group; one of A and B represents a group of the formula
and the other represents a group of the formula
in which R¹ and R² are identical or different and each represents a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, R³ represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group, and X represents a sulfonyl group or a carbonyl group,
and an acid addition salt thereof. The compounds provided by this invention have useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular diseases such as angina pectoris, cerebral circulation disorder and thrombosis.
下式所代表的丙烷衍生物
其中 R 代表低级烷基;A 和 B 中的一个代表式中的一个基团
另一个代表式中的一个基团
其中 R¹ 和 R² 相同或不同,各自代表氢原子、低级烷基、芳基或芳烷基,R³ 代表取代或未取代的低级烷基、取代或未取代的芳基或取代或未取代的杂环基,X 代表磺酰基或羰基、
及其酸加成盐。本发明提供的化合物具有有用的生物活性,如对血管平滑肌的解痉活性和抗血小板聚集活性,可作为治疗心绞痛、脑循环障碍和血栓形成等心血管疾病的药物。
A propane derivative represented by the following formula ##STR1## wherein R represents a lower alkyl group; one of A and B represents a group of the formula ##STR2## and the other represents a group of the formula ##STR3## in which R.sup.1 and R.sup.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, R.sup.3 represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heterocyclic group, and X represents a sulfonyl group or a carbonyl group, and an acid addition salt thereof. The compounds provided by this invention have useful biological activities such as the spasmolytic activity on the vascular smooth muscles and anti-platelet aggregatory activity and are useful as drugs for treating cardiovascular diseases such as angina pectoris, cerebral circulation disorder and thrombosis.