关键词: 卡维地洛, 高血压, 合成, 整体优化

Abstract: Carvedilol，a highly effective antihypertensive drug，not only is a third β-adrenergic receptor antagonist but also can be used to inhibit ?1-adrenoceptor. Recent synthetic routes of carvedilol differ from various starting materials. The synthesis methods of carvedilol are divided into two reaction types，whether the nitrogen atom contains protecting group or not. Here we show the two different reaction types that introducing a protecting group such as benzyl by intermolecular nucleophilic reaction and forming a cyclic amide structure by intramolecular reaction to protect the nitrogen atom. In this paper，we also discovered that using the 4-hydroxy carbonzole as starting material can effectively avoid various byproducts，which significantly improves the yield of carvedilol.

Key words: carvedilol, hypertension, synthesis, global optimization