Synthesis of compounds related to santonin

Proceedings - Mathematical Sciences - Following the methods used in the synthesis of santonin the synthesis of compounds related to santonin has been described.     

Preparation of 3,4-fused-spiro[furan-5(5H),4′-piperidin]-2-one

A general method for the preparation of various 3,4-fused-spiro[furan-5(5H),4′-piperidin]-2-one with high yield is reported. The formation of spiro[furanone-piperidine] structure was achieved by a Suzuki coupling, followed by an iodolactonization reaction.     

A general approach to access 5,6-dihydroindolo-naphthyridine ring system

We report a general approach for the synthesis of 5,6-dihydroindolo-naphthyridine ring system via an intramolecular cyclization of the indole NH to an alkene moiety as the key step.     

Catalytic asymmetric hydrogenation to access spiroindane dimethyl acetic acid

Asymmetric hydrogenation of achiral spiroindene dimethyl acetic acid 2 with 4% of Ru(II)-Mandyphos in acetone produced (S)-spiroindane dimethyl acetic acid 1 in 86% isolated yield and 96.8:3.2 enantiomeric ratio.     

Synthesis of Gossypium hirsutum‐derived silver nanoparticles and their antibacterial efficacy against plant pathogens

Malvaceae and Brassicaceae family crops are economically important; however, their production has been markedly decreased in recent years due to various plant pests. Hence, the search for novel classes of efficient biological approaches continues due to unavailability of precise pesticides. The present study was designed to synthesize, characterize and evaluate the efficacy of silver nanoparticles (AgNPs) obtained using stem extract of Gossypium hirsutum (cotton plant) against plant pathogens Xanthomonas axonopodis pv. malvacearum and Xanthomonas campestris pv. campestris. Biosynthesized AgNPs were characterized using UV–visible spectrophotometry, Dynamic Light Scattering, Scanning Electron Microscopy combined with energy‐dispersive X‐ray analysis and Fourier transform infrared spectroscopy. The synthesized AgNPs were spherical in shape with size ranging from 20 to 100 nm. The characterized AgNPs were investigated for their efficacy against bacterial plant pathogens using the paper disc method. In vitro studies with two concentrations of AgNPs (50 and 100 μg mL^?1) showed zone of inhibition 11.0 ± 1.0 and 12.3 ± 0.5 mm for X. axonopodis pv. malvacearum and 9.7 ± 0.6 and 15.33 ± 1.0 mm for X. campestris pv. campestris. Furthermore, the AgNPs exhibited strong antioxidant activity, and a phytotoxicity study on Vigna unguiculata (cowpea plant) showed no toxicity. Overall, the findings suggest that G. hirsutum stem extract could be efficiently used in the synthesis of AgNPs and showed antimicrobial activity against plant pathogens. Hence, the synthesized nanoparticles could be used to combat plant pathogens in the agriculture sector.     

Late-stage lipidation of fully elaborated tryptophan-containing peptides for improved pharmacokinetics

The late-stage modification of native peptides to alter and/or enhance their properties and functions is attractive but formidably challenging. Peptide lipidation is one of the effective strategies to overcome short half-life and rapid clearance. Herein, we report a late-stage installation of a fatty acid lipid onto fully elaborated peptides, using glucagon as an example, through regio- and chemoselective functionalization of tryptophan with high potency and remarkable in vivo half-life extension.     

Synthesis of β-carbolines from aldehydes and ketones via the α-siloxy α,β-unsaturated esters

We report an efficient method for the synthesis of β-carbolines from α-siloxy α,β-unsaturated esters, which are accessible from a variety of aldehydes and ketones.