查看更多>>摘要：The functionalized benzotriazoles are prepared by palladium catalyzed intramolecular amination of 2bromodiaryltriazene. By screening the reaction conditions, such as ligand, solvent, base and reaction concentration, the optimal reaction conditions were obtained, and 28 functionalized benzotriazole derivatives were successfully prepared up to 99% yield. The method is easy to operate and has good tolerance to diverse functional groups. CO 2021 Elsevier Ltd. All rights reserved.
查看更多>>摘要：Irradiation of 1-acylindole derivatives that possess a vinylcyclopropane moiety at the end of the acyl side chain by a high-pressure mercury lamp through Pyrex glass under sensitization of an aromatic ketone gave the corresponding cyclised products stereoselectively in high yields. The distribution of the products was highly dependent on the substituents on the cyclopropane ring. In the case of a simple cyclopropane, the product was a mixture of ring-expanded cycloheptene-fused indoline and all -cis-fused cyclopropylcyclobutane-fused indoline through [2 + 2] cycloaddition, while cycloheptene-fused indolines were predominantly produced via formal [5 + 2] cyclisation in the case of substituted cyclopropanes. In particular, the product selectivity was substantially high in the case of silylcyclopropane. (c) 2021 Elsevier Ltd. All rights reserved.
Palli, Kishore KumarGhosh, PalashAvula, Shiva KrishnaRao, B. Sridhara Shanmukha...
4页
查看更多>>摘要：Remdesivir, the first drug approved by the FDA to treat COVID-19, is in high demand for patients infected with the SARS-CoV-2 virus. Herein, we report a facile approach minimizing the protecting group manipulations to afford remdesivir in good overall yield. (c) 2021 Elsevier Ltd. All rights reserved.
查看更多>>摘要：We report a novel intramolecular 1,6 oxa-Michael addition on substituted dihydropyridines to obtain 5 and 6 member ring lactones in an one-pot reaction starting from activated pyridinyl propenones, without organic catalysis or presence of bulky groups in the Michael acceptor. A marked dependence on the regioselectivity of ring closure was found, dependent on the propenone used. (C) 2021 Elsevier Ltd. All rights reserved.
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Elsevier