- ZnO nanoparticles-mediated regioselective synthesis of methyl-iV-alkylated 1,2,3-triazole-4-carboxylates
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The 1,2,3-triazoles are versatile synthetic intermediates of many biologically active compounds, and their N-1 substituted analogues are potential pharmaceutically important derivatives. In this study, an efficient regioselective N-alkylation reaction of
- Prabakaran,Khan, Fazlur-Rahman Nawaz,Jin, Jong Sung
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- Some Aspects of the Azide-Alkyne 1,3-Dipolar Cycloaddition Reaction
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Some peculiar features of two most commonly used catalytic systems (Cul and CuSOVsodium ascorbate) controlling the regioselectivity of 1,3-dipolar cycloaddition of azides to terminal alkynes have been studied. Their potentialities, main disadvantages, and limitations have been demonstrated by a number of examples, including reactions of low-molecular-weight azides and alkynes containing heterocyclic substituents. The possibility of using novel reagents in click reactions is discussed.
- Pokhodylo,Tupychak,Shyyka, O. Ya.,Obushak
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p. 1310 - 1321
(2019/11/03)
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of Formula (I) wherein R1, R2, R3, R4 and R5 are defined herein, maintain good activity against NS3 proteases containing clinically relevant genotype 1a R155K and genotype 1b D168V resistance mutations. The compounds are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
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Page/Page column 49
(2011/06/23)
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- HEPATITIS C INHIBITOR COMPOUNDS
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Compounds of the invention, which are macrocyclic peptide analogs containing an acylsulfonamide moiety, maintain good activity against NS3 proteases containing clinically relevant resistance mutations for this class as represented by genotype 1 a R155K, genotype 1 b D168V and genotype 1 a D168V resistance mutations. The compounds of the invention are useful as inhibitors of HCV NS3 protease for the treatment of hepatitis C viral infection.
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Page/Page column 33
(2011/06/23)
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- NOVEL HERBICIDES
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Compounds of formula I: wherein R1, R2, R3, R4, m, R5, R6, n and Y are as defined in claim 1; or N-oxides, salts and optical isomers thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising them and to methods of using them to control plants or to inhibit plant growth.
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Page/Page column 110
(2008/06/13)
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- HERBICIDAL ISOXAZOLINE COMPOUNDS
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Novel compounds of formula (I): wherein R1, R2, R3, R4, m, R5, R6, n and Y are as defined in claim 1; or N-oxides, salts and optical isomers thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to herbicidal compositions comprising them and to methods of using them to control plants or to inhibit plant growth.
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- REACTIONS DES METHYLAZIDE ET PHENYLAZIDE AVEC QUELQUES ALCYNES ET OLEFINES α-NITREES. SYNTHESE REGIOSPECIFIQUE DES 1,2,3 TRIAZOLES
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The reactions of alkynes and α-nitro-olefines with methylazide and phenylazide was studied.In contrast to known reactions with alkynes which are non-regioselective, methylazide and phenylazide react regiospecifically with α-nitro-olefines and give only one type of triazole after elimination of HNO2.These reactions are very useful synthetic approaches to 1,2,3 triazoles.
- Piet, J. C.,Hetet, G. Le,Cailleux, P.,Benhaoua, H.,Carrie, R.
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- 1,3-Dipolar Cycloadditions, 93. - The Astounding Reaction of Dimethyl 2,3-Dicyanofumarate with Diazomethane
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The reaction with excess of diazomethane furnished methyl 4-cyano-1-methylpyrazole-5- and -3-carboxylate (2 and 3) as well as the three N-methyl-1,2,3-triazolecarboxylic esters 4-6.A mechanistic study revealed a poly-step sequence.The initial formation of the pyrazoline 8 proceeded normal.Base catalysis effected an equilibration of trans- and cis-2-pyrazoline, 8(*)12, followed by a fragmentation into methyl 4-cyano-3-pyrazolecarboxylate (26) and methyl cyanoformate (32); a 4H-pyrazole is supposed to be the key intermediate.The final products mentioned above emerged from further reaction of 26 and 32 with diazomethane.
- Huisgen, Rolf,Mitra, Abhijit,Moran, Joaquin Rodriguez
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p. 159 - 170
(2007/10/02)
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- THE ASTOUNDING REACTION OF DIAZOMETHANE WITH DIMETHYL 2,3-DICYANOFUMARATE
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The title reaction afforded the pyrazole derivatives 3 and 4 as well as the N-methyl-1,2,3-triazolecarboxylic esters 5 - 7.The poly-step sequence was clarified; the key intermediates are the 1-pyrazoline 18, the 2-pyrazoline 2, the 4H-pyrazole 12, the pyrazole 22, and methyl cyanoformate.
- Huisgen, Rolf,Mitra, Abhijit,Moran, Joaquin Rodriguez
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p. 2429 - 2436
(2007/10/02)
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