Abstract
A series of novel benzofuran derivatives containing biaryl moiety were designed and synthesized by the Suzuki cross-coupling reactions. The reactions, performed in the presence of K2CO3, EtOH/H2O and Pd(II) complex as catalyst, gave the corresponding products in good to excellent yields. The methodology allows the facile production of heterobiaryl compounds, a unique architectural motif that is ubiquitous in medicinal chemistry.
Highlights
IntroductionA series of novel benzofuran derivatives containing biaryl moiety were designed and synthesized by the Suzuki cross-coupling reactions
Engineering Research Center, College of Chemistry and Chemical Engineering, Hainan University, Institute of Coordination Catalysis, College of Chemistry and Bio-Engineering, Yichun University, Tel.: +86-079-5320-0535 (M.G.)
This paper describes the Suzuki reaction applied to the synthesis of novel benzofuran derivatives Molecules 2018, 23, 2450 containing biaryl moiety
Summary
A series of novel benzofuran derivatives containing biaryl moiety were designed and synthesized by the Suzuki cross-coupling reactions. A representative complex of the natural 3-deformylated 2-arylbenzo[b]furan is ailanthoidol in (Figure 1, 1), which was isolated from the chloroform-soluble fraction of the tree of Zanthoxylum ailanthoides, was found to have a broad range of biological activities such as anticancer [8], immunosuppressive [9,10,11], antivirus [12,13,14,15], antioxidant [10,11], antifungal [16], and antifeedant activities [17]. The results showed that three structurally modified derivatives (Figure 1, 3a–3c) inhibited significantly the production of inflammatory mediator nitric oxide without showing cytotoxicity. Nishi and coworkers synthesized a series of 2-phenylbenzofuran derivatives with both carboxy and 5- or
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