The aim of the study was to develop, synthesis, and characterise a novel 1,3,5-trisubstituted-2-pyrazolines derivative, as well evaluate its antifungal activity. reaction chalcone derivatives with succinic hydrazide in presence pyridine yielded 1,3,5-tri-substituted-2-pyrazolines derivatives. Total 20 compounds has been synthesized characterized by IR, 1HNMR mass spectral analysis. Antifungal a...

The reaction of adamantane-1-carbohydrazide (1) with heterocyclic aldehydes, namely 5-(4-chlorophenyl)isoxazole-3-carboxaldehyde (2a), 5-(4-methylphenyl)isoxazole-3-carboxaldehyde (2b), 5-(4-methoxyphenyl)isoxazole-3-carboxaldehyde (2c), 1H-imidazole-2-carboxaldehyde and 2-butyl-4-chloro-1H-imidazole-5-carboxaldehyde, in ethanol, yielded the corresponding N'-heteroarylidene-1-adamantylcarbohydr...

The efficient synthesis of enantiopure, trisubstituted cryptophane-A derivatives, organic host molecules with unusually high xenon affinity, is reported. Synthesis and chromatographic separation of (±) tri-Mosher's acid substituted cryptophane diastereomers gave ready access to the enantiopure cryptophanes, which are critical components in the design of enantiomerically pure (129)Xe biosensors....

We have discovered a mild, catalytic protocol for the regio- and stereoselective synthesis of trisubstituted allyl diarylphosphonates from the corresponding disubstituted allyl silyl ethers, circumventing the challenges related to the preparation and availability of stereodefined trisubstituted olefins. A closely related arylation reaction was also discovered during the methodology development....

An extension of our methodology on solid-phase synthesis of 3,4,5-trisubstituted-1,2,4-triazoles under mild conditions has been developed. Firstly, the resin-bound acylhydrazine is reacted with orthoesters to provide resin-bound 1,3,4oxadiazoles. Secondly, condensation of 1,3,4-oxadiazoles resin with the corresponding arylamines hydrochloride to form the resin-bound triazoles. 3,4,5-Trisubstitu...

A strategy for the preparation of semisynthetic copper(II)-based catalytic metalloproteins is described in which a metal-binding bis-imidazole cofactor is incorporated into the combining site of the aldolase antibody 38C2. Antibody 38C2 features a large hydrophobic-combining site pocket with a highly nucleophilic lysine residue, Lys(H93), that can be covalently modified. A comparison of several...

One-pot Fischer indolisation indole N-alkylation enables straightforward, rapid synthesis of structurally-diverse 1,2,3-trisubstituted indoles from simple, widely-available precursors.

the reaction of p-diketones 1 with phenyl hydrazine afforded 5-aryl-3-(1- methyl-5-nitro-2-imidazoly1)-1-phenylpyrazole (2) and 3-aryl-5-(1-methyl-5- nitro-2-imidazoly1) -1-phenylpyrazole (3). the reaction of diketones (1) with urea in the presence of p-toluenesulfonic acid gave 4-(or 6-)aryl-6-(or 4-)(1-methyl- 5-nitro-2-imidazolyl)-1-(lh)pyrimidones (4). the structures of all compounds were c...

C–H olefination of alkynes has been realized as an efficient approach to access axially chiral trisubstituted olefins, where two classes arenes have identified.