- Regiodivergent synthesis of vinyl trifluoromethansulfonates γ/δ lactones: Via 1,6 addition/intramolecular one-pot annulation of 1,4-dihidropyridines derivated from pyridinyl propenones
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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
- álvarez-Toledano, Cecilio,Ballinas-Indili, Ricardo,Carmona-Reyes, Genaro,Sánchez-Vergara, María Elena,Toscano, R. Alfredo
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supporting information
(2021/12/29)
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- TBHP/Cu(OAc)2 mediated oxidation of pyrazolines: A convenient method for the preparation of pyrazoles
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An efficient and simple oxidative protocol has been developed for the preparation of pyrazoles from pyrazolines mediated by TBHP/Cu(OAc)2 at room temperature. The present protocol has been successfully applied for the preparation of various pyrazole compounds from heterocyclic pyrazolines.
- Kolla, Sai Teja,Somanaboina, Ramya,Bhimapaka, China Raju
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supporting information
p. 1425 - 1432
(2021/02/27)
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- Potassium Base-Catalyzed Michael Additions of Allylic Alcohols to α,β-Unsaturated Amides: Scope and Mechanistic Insights
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We report herein the first KHMDS-catalyzed Michael additions of allylic alcohols to α,β-unsaturated amides through allylic isomerization. The reaction proceeds smoothly in the presence of only 5 mol% of KHMDS to afford a variety of 1,5-ketoamides in high yields. Mechanistic investigations, including experimental and computational studies, reveal that the KHMDS-catalyzed in-situ generation of the enolate from the allylic alcohol through a tunneling-assisted 1,2-hydride shift is the key to the success of this transformation. (Figure presented.).
- Kurouchi, Hiroaki,Sai, Masahiro
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supporting information
p. 3585 - 3591
(2021/06/27)
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- Combination of the Claisen-Schmidt reaction, the Michael addition, and the Hantzsch reaction in the synthesis of 2,6′-bis-aryl-3,4′-bipyridines
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Pyridine-3-carbaldehyde reacted with 1-(aryl)ethan-1-ones to give 1,5-diaryl-3-(pyridin-3-yl)pentane-1,5-diones, which were further converted to 2′,6′-bis-aryl-3,4′-bipyridines.
- Gerasimov, O. A.,Gubaidullin, A. T.,Mamedov, V. A.,Mustakimova, L. V.
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p. 517 - 524
(2020/04/17)
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- Superelectrophilic nazarov cyclizations with N-heterocycles
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A series of Nazarov cyclizations has been studied involving N-heterocyclic-substituted 1-arylprop-2-en-1-one derivatives (aza-chalcones). Superacid catalyzed reactions of these derivatives provide good yields of heterocyclic-substituted 1-indanones. A mec
- Vuong, Hien,Amadou, Harouna,Stentzel, Michael R.,Klumpp, Douglas A.
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- Unsaturated ketone compound as well as preparation method and application thereof
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The present invention relates to a novel GPR52 antagonist. Specifically, the invention relates to an unsaturated ketone compound, a pharmaceutically acceptable salt, a stereoisomer or a prodrug molecule thereof, and a method for preparing a pharmaceutical composition thereof. The invention further relates to the use of the GPR52 antagonist as an orphan G protein coupled receptor GPR52 antagonist,and further relates to the use of the GPR52 antagonist in the preparation of drugs for preventing and treating Huntington's disease.
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Paragraph 0219-0222; 0259-0261
(2020/10/30)
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- Tuning the Product Selectivity of the α-Alkylation of Ketones with Primary Alcohols using Oxidized Titanium Nitride Photocatalysts and Visible Light
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The direct α-alkylation of ketones with alcohol to synthesize important α-alkylated ketones and enones is an attractive procedure for C-C bond formation. High reaction temperatures are always needed for heterogeneous catalysis using non-noble metals, and switching product selectivity in one catalysis system remains a great challenge. In the present study, a visible-light-driven procedure for this reaction is proposed, using oxidized TiN photocatalysts under mild conditions, whereby the product selectivity can be well-tuned. Oxidized TiN photocatalysts with tunable surface N/O ratios were successfully synthesized through the facile and flexible thermal oxidation treatment of low-cost TiN nanopowder. The α-alkylation of acetophenone with benzyl alcohol to form the two important compounds chalcone and dihydrochalcone occurred even at room temperature and almost complete conversion was achieved at 100 °C under visible light. The proportion of the two products can be well-tuned by switching the surface N/O ratio of the synthesized photocatalysts. Visible light is demonstrated to affect the surface N/O ratio of the photocatalysts and contribute to tuning the product selectivity. Light intensity and action spectrum study proves that the generation of energetic charge carriers results in the observed activities under visible light, based on interband transitions of TiN or the ligand-to-metal charge transfer (LMCT) effect of the surface complex formed on TiO2. Thermal energy can be coupled with light energy within this photocatalytic system, which will facilitate the full use of solar energy. Different sequential reaction mechanisms on TiN and TiO2 are proposed to be responsible for the tunable product selectivity. The wide reaction scope, the fine conversion at a low light intensity, and the favorable reusability of photocatalysts prove the great application potential of this visible-light-driven procedure for the α-alkylation of ketones with primary alcohols.
- Li, Peifeng,Su, Haijia,Xiao, Gang,Zhao, Yilin
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p. 3640 - 3649
(2020/04/09)
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- Mechanistic insights into the role of PC- and PCP-type palladium catalysts in asymmetric hydrophosphination of activated alkenes incorporating potential coordinating heteroatoms
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The impact of the structural attributes of chiral PC- and PCP-palladium catalysts was investigated in the asymmetric hydrophosphination of various heterocycle-functionalized enone substrates. Due to the architecture of the catalysts, they are confronted w
- Yang, Xiang-Yuan,Jia, Yu-Xiang,Tay, Wee Shan,Li, Yongxin,Pullarkat, Sumod A.,Leung, Pak-Hing
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supporting information
p. 13449 - 13455
(2016/09/04)
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- A magnetic solid sulfonic acid modified with hydrophobic regulators: An efficient recyclable heterogeneous catalyst for one-pot aza-Michael-type and Mannich-type reactions of aldehydes, ketones, and amines
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Two convenient green protocols for the synthesis of β-amino ketones have been developed which involve one-pot aza-Michael-type and Mannich-type reactions of a series of aldehydes, ketones, and amines in the presence of a catalytic amount of the magnetic solid sulfonic acid catalyst, Fe3O4@SiO2@Me&Et-PhSO3H, at room temperature. The catalyst can be reused four times without loss of activity.
- Movassagh, Barahman,Tahershamsi, Leili,Mobaraki, Akbar
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p. 1851 - 1854
(2015/03/30)
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- An efficient combination of microwave dielectric heating and the use of solid-supported triphenylphosphine for Wittig reactions
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Figure presented Reaction condition: 150°C, 5 min. Olefins could be formed in an efficient way by the use of stable ylides in just a few minutes using microwave dielectric heating. The drawback with the Wittig reaction in solution phase is the formation of 1 equiv of triphenylphosphine oxide. To avoid this, the corresponding protocol using the efficient combination of solid-supported triphenylphosphine and microwave dielectric heating was developed. An even more efficient one-pot three-step Wittig reaction was also developed.
- Westman, Jacob
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p. 3745 - 3747
(2007/10/03)
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- Synthesis and antimycobacterial activity of some N1-[1-[3-aryl-1- (pyridin-2-, 3-, or 4-yl)-3-oxo]propyl]-2-pyridinecarboxamidrazones
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N1-[1-[3-aryl-1-(pyridin-2-,3-, and 4-yl)-3-oxo]propyl]-2- pyridinecarboxamidrazone derivatives were synthesized and tested for their in vitro antimycobacterial activity. Some compounds showed interesting activity against a strain of Mycobacter
- Mamolo, Maria Grazia,Falagiani, Valeria,Vio, Luciano,Banfi, Elena
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p. 761 - 767
(2007/10/03)
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