查看更多>>摘要：Organocatalytic electrophilic amination of benzoyl butyrolactones with azodicarboxylates was demonstrated to highly efficiently prepare quaternary carbon stereocenter-bearing alpha-amino-gamma-butyrolactones, key framework in numerous bioactive compounds. The squaramide C3 realized the highest yield (99%) and enantioselectivity (93%).(c) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：A conceptually new strategy has been described for the mild and environmentally friendly preparation of 6-naphthylamines via Tf2O-activated cyclization of amides with alkynes. Both terminal and internal alkynes could serve as effective nucleophiles in this transformation. This chemistry features simple reaction conditions, high chemoselectivities, wide substrate scope, and offers a practical approach to polysubstituted 6-naphthylamines.(C) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：We report a significantly faster and greener technique for parallel chemical reaction work-ups. Unlike conventional liquid-liquid extraction-based work-ups, we use a cylindrical-shaped polyurethane foam 'sponge' as a "foam solvent" to extract organic products from a quenched aqueous reaction mixture. The foam, loaded with organic products, serves as a convenient input for flash chromatographic separa-tions (and, therefore, we call it 'Fast2Flash'). This technique displayed a high efficiency for separating an organic phase from an aqueous phase, eliminating tedious and solvent-wasting liquid-liquid extractions and emulsion formation. Moreover, parallel and automatic operations are facilitated.(c) 2022 Published by Elsevier Ltd.
查看更多>>摘要：An efficient and mild cascade reaction of acryloylbenzamides with N-hydroxyphthalimide (NHPI) esters is disclosed. It goes through radical addition and subsequent cyclization to give 4-alkylated isoquinolinediones in the presence of visible light and photocatalyst Ir[dF(CF3)ppy(2)](dtbbpy)PF6.(C) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：Four manzamine-type alkaloids, including a novel compound, manzamine A 27 -N-oxide (1), as well as three previously reported analogues, manzamines A (2), E (3), and 8-hydroxy-manzamine A hydrochloride (4) were isolated from the organic extract of marine sponge Neopetrosia proxima. The structures of 1-4 were determined based on spectroscopic data and 1 was proved to be the first manzamine alkaloid possessing the 27 -N-oxide moiety. The structures, including absolute configurations of 1 and 4, were established using single X-ray diffraction analysis. Compounds 1-3 showed cytotoxicity towards Hep3B (IC50 = 10.1, 3.8, 5.8 mu M), SC-M1 (IC50 = 11.7, 3.7, 5.6 mu M) and MCF-7 (IC50 = 10.6, 4.1, 4.2 mu M) tumor cells.& nbsp;(C) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：The palladium-catalyzed cross-couplings of alkylindium reagents with diaryliodonium salts proceeded efficiently in the presence of tetrakis(triphenylphosphine)palladium [Pd(PPh3)(4)], 2-dicyclohexylphosphino-2',6'-dimethoxybiphenyl (SPhos), lithium tert-butoxide, and lithium chloride in DMA/THF (1:1) at 100 C, leading to the corresponding cross-coupling products in moderate to good yield with broad substrate scope and wide functional group tolerance. (C)& nbsp;2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：The dibenzo[d,d'']benzo[1,2-b:4,3-b']difuran skeleton exhibits a V-shape, which is highly desirable in semi-conductor applications. In this study, we synthesized V-shaped highly fused phthalonitrile derivatives and investigated the use of peripheral substituents to tune the crystal packing of the compounds. The palladium-mediated double C-H activation of 3,6-bis(aryloxy) phthalonitriles afforded 6,7dicyano-dibenzo[d,d'']benzo[1,2-b:4,3-b']difurans. The peripheral substituents affected the packing structure of the single crystals, particularly in the compounds with nBu groups, in which two-dimensional (2D) layered structures were observed. The peripheral substituents also affected the optical properties in the solution, film, and powder states. The layered structure suggested an improvement in the mobilities of organic semiconductors.(C) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：A light-driven, catalyst-and additive-free photoenolization/nucleophilic addition reaction for the synthesis of 3-benzyl-3-hydroxyindolin-2-ones is presented. In this reaction, 2-methylbenzophenones undergo light-induced enolization process to afford hydroxy-o-quinodimethanes (hydroxy-o-QDMs), which are then immediately captured by the electrophilic isatins. The reaction utilizes green and clean light energy to realize the C-H activation of the inert benzyl position of 2-methylbenzophenones. This method tolerates a wide scope of substrates and provides concise access to a series of novel 3-benzyl3-hydroxyindolin-2-ones with 60-99% yields.(c) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：We report herein the synthesis of functionalized styrenes via palladium-catalyzed Suzuki-Miyaura cross-coupling reaction between aryl ketone derivatives and potassium vinyltrifluoroborate. The employment of pyridine-oxazoline ligand was the key to the cleavage of unstrained C-C bond. A variety of functional groups and biologically important moleculars were well tolerated. The orthogonal Suzuki-Miyaura cou-pling demonstrated the synthetic practicability.(c) 2022 Elsevier Ltd. All rights reserved.
查看更多>>摘要：An efficient transition-metal-free method for the synthesis of 5-trifluoromethyltetrazoles from arenediazonium tetrafluoroborates is reported, which relies on the use of trifluoroacetaldehyde N-tosylhydra-zone as a convenient 2,2,2-trifluorodiazoethane source. The reaction proceeds in good to excellent yields and shows a high functional group tolerance.CO 2022 Elsevier Ltd. All rights reserved.
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