Recent Advances in the Synthesis of Fused Heterocyclic Compounds and Their Antitumor Activities
Year: 2023
Type: article
Abstract: The unique physicochemical properties invest fused heterocyclic compounds with wide applications in the synthesis of natural products, drugs, superconducting materials, energy storage materials, polymer materials, organic dyes, etc.In recent years, the rapid development of transition metal-catalyzed reactions of unsaturated hydrocarbons has developed rapidly.Owing to the advantages of high step-and atom-economy, easy availability of raw starting materials, and efficient construction of carbon-carbon bonds or/and carbon-hetero bonds, it is a vital way to synthesize fused heterocyclic compounds.Herein, the recent progress on the reaction development of transition metal-catalyzed cyclizations involving unsaturated hydrocarbons for the synthesis of fused heterocyclic compounds including benzofurans, indoles, quinolines in the last five years has been summarized, as well as their applications in the field of medicinal chemistry with antitumor activities.Keywords unsaturated hydrocarbons; transition metal-catalysis; fused heterocyclic compounds; antitumor activity 稠杂环化合物是指苯环与杂环或杂环与杂环稠合 在一起的化合物(如吲哚、喹啉、嘌呤等 [1][2][3] ).由于稠杂 环化合物通常具有独特的生物活性、低毒性和高内吸收 性 [4][5][6][7] , 经常用作医药活性分子和农药的结构单元 [8][9][10][11] .到目前为止, 全球销售额前 200 的药物中许多化合物含 有稠杂环结构(图 1).例如艾乐妥是一种凝血因子 Xa 的 抑制剂抗凝剂, 能用于髋关节或膝关节的择期置换术; 瑞复美可以与地塞米松合用治疗多发性骨髓瘤; 依鲁替 尼作为一种小分子 BTK 抑制剂, 可以用于治疗慢性淋 巴细胞白血病(CLL)和套细胞淋巴瘤(MCL)等.此外, 稠杂环化合物还易于进行结构修饰, 通过引入各种功能 基, 可应用于天然产物全合成、超导材料、储能材料、 高分子材料以及有机染料等领域.因此, 其合成研究一 直是有机化学的热点.
Authors: Kanghui Duan, Junlong Tang, Wanqing Wu
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: bronze
Award: G3754285485
OpenAlex ID: W4328022608