兼有α受体阻滞作用的β受体阻滞剂的合成

SYNTHESIS OFβ-ADRENERGIC BLOCKING AGENT WITHα-ADRENERGIC BICOCKING ACTIVITY

α-受体阻滞剂和β-受体阻滞剂均可用作抗高血压药物。我们曾根据拚合原理,设计了一类化合物Ⅰ,它具有降压活性和α-受体阻滞作用,但β-受体阻滞作用不明显。在β-受体阴滞剂的基本结构Ⅱ中,保持仲胺结构很重要。

1-Phenoxy-3(2-(4-benzoyl-1-piperazinyl) ethylaminyl)-2-propanol hydrochloride (Ⅲa) was designed and synthesized as an β-adr-energic blocking agent with α-adrenergic blockingactivity. The structure of Ⅲa was determined by IR, MS, 'H—NMR and ^(18)C—NMR.