- Copper-catalyzed regioselective 2-amination of o-haloanilides with aqueous ammonia
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An efficient Cu(II)-vasicine catalytic system has been developed for intramolecular C[sbnd]N bond formation. In this way, regioselective 2-amination of o-haloanilides with aqueous ammonia in EtOH has been achieved. This strategy provides several advantages, such as good regioselectivity, high yields and functional group tolerance.
- Tang, Yan-Ling,Li, Mei-Ling,Gao, Jin-Chun,Sun, Yun,Qu, Lu,Huang, Feng,Mao, Ze-Wei
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supporting information
(2021/04/02)
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- Azobenzene-diamides as Photopharmacological Ligands for Insect Ryanodine Receptor
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Photoresponsive ligands are powerful tool compounds for studying receptor function with spatiotemporal resolution. However, to the best of our knowledge, such a ligand is not available for the ryanodine receptor (RyR). Herein, we present a photochromic ligand (PCL) for insect RyR by decorating chlorantraniliprole (CHL) with photoswitchable azobenzene (AB). We demonstrated that one potent ligand, named ABCHL13, shows light-induced reversible trans-cis isomerization and 3.5-fold insecticidal activity decrease toward oriental armyworm (Mythimna separata) after UV-light irradiation, that is, trans-ABCH13 has higher activity than the cis-ABCH13. ABCHL13 enables optical control over intracellular Ca2+ release in dorsal unpaired median (DUM) neurons of M. separata and American cockroach (Periplaneta americana) and cardiac function of P. americana. Our results provide a first photopharmacological toolkit that is applicable to light-dependent regulation of RyR and heart beating.
- Chen, Meijun,Li, Yuxin,Shao, Xusheng,Wang, Long,Xia, Shanshan,Xu, Zhiping
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p. 14409 - 14416
(2020/12/22)
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- Facile synthesis of thiazoles via an intramolecular thia-Michael strategy
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A mild and efficient method for the synthesis of substituted thiazoles is reported via one-pot N-desilylation, thioacylation/oxythioacylation/thiothioacylation followed by thia-Michael cycloisomerisation. This method has a general applicability to introdu
- Sasmal, Pradip K.,Sridhar,Iqbal, Javed
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p. 8661 - 8665
(2007/10/03)
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