利用微波輔助合成一系列具有特殊藥性色烯類化合物 ;利用簡單且高效率的方式藉由一鍋化合成3-羥基與3-胺基黃酮類衍生物

Abstract

本論文主要分為兩部分，第一部分是在探討藉由微波反應器輔助且在不添加催化劑條件下，將硫醇類化合物、丙二腈與2-羥基苯甲醛合成屬於著名先驅藥物之一的Chromenopyridine為骨架之化合物，其具有多種生物活性及藥理作用。 第二部分利用微波反應器透過一鍋化合成具生物活性3-氫氧基及3-氨基-2-苯基-4H-色烯-4-酮類化合物，本實驗主要是由3-硝基-2H-色烯類衍生物經反應後獲得中間物diethyl-4-ethoxy-3-(hydroxyimino) -2-phenylchroman-4-ylphosphonatey在乙醇作為溶劑於迴流條件下獲得產物。中間物以及產物結構已由XRD被確認。

The first part of this dissertation describes the microwave assisted , one pot catalyst-free synthesis of chromenopyridine derivatives which achieved from the reaction of thiols, malononitrile and salicyaldehyde derivatives . The chromenopyridine derivatives framework is one of the well know privileged medicinal scaffolds diverse biological and pharmacological. The second part describes microwave promoted a novel and highly convenient approach for one-pot synthesis of 3-hydroxy and 3-amino-2-phenyl-4H-chromen-4-one was achieved from 3-nitro -2H-chromene derivatives via diethyl-4-ethoxy-3-(hydroxyimino) -2-phenylchroman-4-ylphosphonate in refluxing ethanol was developed. The structures of the prepared compounds were characterized by XRD method. The generality of this reaction was demonstrated by synthesizing an array of 3-hydroxy and 3-amino-2-phenyl-4H-chromen-4-one derivatives.