Facile Synthesis and Biological Evaluation of New Thieno[2,3‐g]indolizine Derivatives

Abstract

An effective approach to the synthesis of thieno[2,3‐g]indolizine derivatives has been developed. A wide variety of reagents such as unsaturated aldehydes, methylvinylketone, esters of acrylic acid, maleic anhydride, methyl propiolate, dimethyl and diethyl acetylenedicarboxylates in the construction of functionally diverse rarely encountered tricyclic system has been used. A high number of structurally various thieno[2,3‐g]indolizines has been obtained in domino reactions with medium and high yields, the influence of solvents on the course of transformations has been studied, and the presence of moderate cytotoxic activity for a number of compounds has been established.

Synthetic Strategies for the Construction of Indolizines and Indolizine‐fused Compounds: Thienoindolizines and Indolizinoindoles

“…[72] Voskressensky's group showed that the interaction of aroyl formic acids 227 with 2-(thiophen-2-yl)ethylamine 226, and further refluxing of the product with POCl 3 led to the formation of compounds 228 in 65-83 % yield (Scheme 70). [73] The resulting 4-aroyl-6,7-dihydrothieno[3,2-c]pyridines 228 were studied in the domino-reactions with alkenes and alkynes containing electron-deficient groups.…”

Efficient Solvent-Free Synthesis of Indolizines Using CuBr Catalyst from Pyridine, Acetophenone, and Electron-Deficient Alkenes

“…Boruah's group synthesized indolizines by using pyridine, bromoacetophenone, and alkyne under microwave conditions [21]. The aforementioned synthesis methods have established a solid foundation for the development and application of indolizine derivatives [22][23][24][25]. However, research on indolizine is still in its early stages.…”