Study On Synthesis Of Atenolol And Derivatives Of β-Adrenergic Receptor Blocking Agent

Atenolol is a new type ofβ-adrenergic receptor blocking agent, and it possesses striking drug action of depressing blood pressure and slowering heart rate clinically. In this paper, the aim of this experimentation is to find a more activity and lower toxic and less side effectβ-adrenergic receptor blocking agent, so two kinds of novel atenolol series derivative compounds: 2-(4-(3-butylamino)-2-hydroxypropoxy)- phenyl)acetamide and 2-(4-(3-(tert-butylamino)-2-hydroxypropoxy)phenyl)- acetamide were successfully synthesized through experimentation design. That not only provides a material base for medication activity screening, but also offers a synthesis reference method for others analogic series compounds.This paper synthesized new intermediate 2-(4-(allyloxy)phenyl)acetamide, from addition 2-(4-hydroxyphenyl)-acetamide and 3-bromoprop-1-ene to the ethanol solution with sodium hydroxide, reaction by heat reflux, at last, obtainment 2-(4-(allyloxy)phenyl)acetamide with higher yield.The status ofβ-adrenergic receptor blocking agent was introduced and studied. Total synthesis ofβ-blocking agent atenolol was studied, and the synthetic process of atenolol was optimized. (S)-atenolol was synthesized simply and efficiently from 2-phenylacetonitrile through 5 steps and the total yield was 20.8%.The synthetic condition of intermediate 2-(4-nitrophenyl)acetonitrile was optimized through different sequence of reactant addition. In the preparation of...