- Facile one-pot multicomponent synthesis of highly functionalized tetrahydropyridines using thiamine hydrochloride as an organocatalyst
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Thiamine hydrochloride (VitB1) has been found to be an efficient catalyst for the multicomponent synthesis of highly functionalized tetrahydropyridines from the reaction of β-ketoester, aromatic aldehydes and anilines. VitB1 is easily available, cheap, and eco benign.
- Singh, Sandeep,Gupta, Annah,Kapoor, Kamal K.
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- Graphene oxide: A carbocatalyst for the one-pot multicomponent synthesis of highly functionalized tetrahydropyridines
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A simple, straightforward and efficient methodology is described for the synthesis of polysubstituted tetrahydropyridine via one-pot multicomponent reaction of β-ketoester, aldehyde and aniline in presence of catalytic amount of graphene oxide in acetonitrile. Graphene oxide is a versatile carbocatalyst and this is the first report on its application in a five component reaction. Good yield, usage of readily available starting material, operational simplicity, easy work-up and eco-friendly re-usable catalyst are the key features of this protocol.
- Gupta, Annah,Kaur, Ramneet,Singh, Deepika,Kapoor, Kamal K.
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p. 2583 - 2587
(2017/06/13)
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- Ecofriendly and facile Nano ZnO catalyzed solvent-free enamination of 1,3-dicarbonyls
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Nano zinc oxide (Nano-ZnO) was explored as a reusable catalyst for the enamination of 1,3-dicarbonyls using diverse amines. To make the process environmentally viable, the reaction was carried out under solvent-free conditions and found to give good yield of desired products. The catalyst was characterized by various analytical techniques such as UV-spectroscopy, XRD, and TEM. The catalyst was found to be reusable up to four catalytic cycles without any appreciable loss in activity.
- Indulkar, Utkarsha U.,Kale, Sandip R.,Gawande, Manoj B.,Jayaram, Radha V.
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supporting information; experimental part
p. 3857 - 3860
(2012/08/27)
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- N1-{4-[(10S)-Dihydroartemisinin-10-oxyl]}phenylmethylene-N 2-(2-methylquinoline-4-yl)hydrazine derivatives as antiplasmodial falcipain-2 inhibitors
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A series of N1-{4-[(10S)-dihydroartemisinin- 10-oxyl]}phenylmethylene-N2-(2-methylquinoline-4-yl) hydrazine derivatives 9a-9n possessing 4-quinolylhydrazone and artemisinin cores were herein synthesized and evaluated for their activities against cysteine protease falcipain- 2 of Plasmodium falciparum. The structures were clearly confirmed by elemental analysis, 1H NMR, and mass spectra. The pharmacological results indicated that all compounds showed excellent activity against recombinant falcipain-2 (IC50 = 0.15-2.28 μM). The best one of this series was compound 9d (IC50 = 0.15 μM). The molecular docking results showed that the compound 9d made close contact with the key active site of cysteine protease falcipain-2.
- Luo, Wei,Liu, Yang,Wang, Jian,Guo, Chun,Lu, Wei-Qiang,Cui, Kun-Qiang
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p. 3073 - 3079,7
(2020/08/20)
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- A facile, chemoselective and eco-friendly solid phase synthesis of enaminones catalyzed by L-Proline
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A facile and chemoselective method for the synthesis of enaminones by the reaction of aromatic primary amines with various β-ketoesters in the presence of L-proline as activator under solid phase is described. The reactions are promoted by the catalyst in short time (5-6 min) under ambient conditions, without any side products.
- Bhupathi, Raja S.,Devi, B.Rama,Dubey
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experimental part
p. 5521 - 5524
(2012/07/13)
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