Expedient Organocatalytic Syntheses of 4-Substituted Pyrazolidines and Isoxazolidines [PDF]
The efficient organocatalytic synthesis of heterocyclic systems of biological relevance is a subject of growing interest. We have found that the pyrrolidine/benzoic acid-catalyzed reaction of α-substituted propenals such as methacrolein, 2-benzylpropenal
Tarek Yousfi +4 more
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Trifluoroethanol-assisted asymmetric propargylic hydrazination to α-tertiary ethynylhydrazines enabled by sterically confined pyridinebisoxazolines [PDF]
We report the highly enantioselective Cu-catalyzed asymmetric propargylic substitution (APS) of α-tertiary propargylic electrophiles using hydrazines and hydroxylamines as a fruitful strategy to access multifunctional α-tertiary hydrazines or ...
Yi Gong +10 more
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Copper-catalysed enantioconvergent N-alkylation of hydrazines with racemic α-haloamides to access enantioenriched hydrazines [PDF]
Chiral hydrazines are important building blocks in chiral drug molecules, N-amino peptides, and aza-heterocycles. The catalytic enantioconvergent N-alkylation of readily available hydrazine derivatives with various racemic alkyl halides offers a highly ...
Nan Li +6 more
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Chemoselective synthesis of 1,3,4-thiadiazoles from acyl hydrazines and nitroalkanes using elemental sulfur [PDF]
Substituted 1,3,4-thiadiazoles find extensive use in pharmaceutical, agricultural, and materials chemistry. The incorporation of adaptable heterocyclic pharmacophores results in tunable hybrid molecules with diverse medicinal properties.
Xiaonan Wang +6 more
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Direct Cyclization/Chlorination Strategy of Hydrazines for Synthesis of 4-Chloropyrazoles by TCCA [PDF]
A new method for synthesis of various 4-chloropyrazoles through the direct cyclization/chlorination of hydrazines by using 1,3,5-trichloroisocyanuric acid (TCCA) as both oxidant and chlorinating agent under mild conditions has been proposed. Based on the
Qingfu Deng +3 more
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Synthesis of 1,2,3-triazoles containing an allomaltol moiety from substituted pyrano[2,3-d]isoxazolones via base-promoted Boulton–Katritzky rearrangement [PDF]
For the first time, the interaction of aroyl containing pyrano[2,3-d]isoxazolone derivatives with various hydrazines was studied. It was shown that the considered process includes formation of corresponding hydrazones followed by Boulton–Katritzky ...
Constantine V. Milyutin +2 more
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Synthesis and Characterization of Novel Methyl (3)5-(N-Boc-piperidinyl)-1H-pyrazole-4-carboxylates
Series of methyl 3- and 5-(N-Boc-piperidinyl)-1H-pyrazole-4-carboxylates were developed and regioselectively synthesized as novel heterocyclic amino acids in their N-Boc protected ester form for achiral and chiral building blocks.
Gita Matulevičiūtė +9 more
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In silico evaluation of various regioisomeric 5- and 3-hydroxy-substituted alkyl 1-aryl-1H-pyrazole-4-carboxylates and their acyclic precursors yielded promising results with respect to their binding in the active site of dihydroorotate dehydrogenase of ...
Luka Vah +8 more
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N-Sulfonyl amidines are developed from a Cu-catalyzed three-component reaction from sulfonyl hydrazines, terminal alkynes and sulfonyl azides in toluene at room temperature.
Yu Zhao +3 more
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Organic solvent-free synthesis of sulfonyl hydrazides in water
An organic solvent-free synthesis of sulfonyl hydrazides has been achieved in water. The reactions of equimolar amount of sulfonyl chlorides and hydrazines afforded a series of substituted sulfonyl hydrazides at 60 °C for 1 h in water as a solvent in ...
Shizuki Noda, Shinji Tanimori
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