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1.
J Org Chem ; 85(15): 10271-10282, 2020 08 07.
Artigo em Inglês | MEDLINE | ID: mdl-32664730

RESUMO

Herein, we describe a method for the synthesis of aryl-(het)aryl ketones by Rh(III)-catalyzed direct coupling between quinoline-8-carbaldehydes and (het)arylboronic acids. The method has a broad substrate scope, a high functional group tolerance, and uses commercially available starting materials. Scale-up of the reaction and subsequent synthesis of tubulin polymerization inhibitor demonstrated its utilities. A plausible mechanism was proposed on the basis of the fact that a stable cycloacylrhodium intermediate complex could be used as catalyst, and the complex reacted stoichiometrically with (het)arylboronic acids.


Assuntos
Quinolinas , Ródio , Ácidos Borônicos , Catálise , Cetonas
2.
Chemistry ; 24(9): 2065-2069, 2018 Feb 09.
Artigo em Inglês | MEDLINE | ID: mdl-29210122

RESUMO

Nitrogen-containing heteroarene motifs are found in numerous pharmaceuticals, natural products, and synthetic materials. Although several elegant methods for synthesis of these compounds through dehydrogenation of the corresponding saturated heterocycles have been reported, some of the methods are hampered by long reaction times, harsh conditions, and the need for catalysts that are not readily available. This work reports a novel method for dehydrogenation of N-heterocycles. Specifically, O2.- generated in situ acts as the oxidant for N-heterocycle substrates that are susceptible to oxidation through a hydrogen atom transfer mechanism. This method provides a general, green route to N-heteroarenes.

3.
Bioorg Med Chem Lett ; 24(22): 5228-33, 2014 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-25442317

RESUMO

By drawing the creation ideas of botanical pesticides, a series of tetrahydro-ß-carboline-3-carboxylic acid derivatives were designed and synthesized, and first evaluated for their anti-TMV, fungicidal and insecticidal activities. Most of these derivatives exhibited good antiviral activity against TMV both in vitro and in vivo. Especially, the activities of compounds 8 and 15 in vivo were higher than that of ribavirin. The compound 8 exhibited more than 70% fungicidal activities against Cercospora arachidicola Hori, Alternaria solani, Bipolaris maydis, and Rhizoctonia solani at 50mg/kg, compounds 16 and 20 exhibited more than 60% insecticidal activities against Mythimna separate and Ostrinia nubilalis.


Assuntos
Antivirais/síntese química , Carbolinas/síntese química , Fungicidas Industriais/síntese química , Inseticidas/síntese química , Extratos Vegetais/síntese química , Vírus do Mosaico do Tabaco/efeitos dos fármacos , Antivirais/isolamento & purificação , Antivirais/farmacologia , Carbolinas/isolamento & purificação , Carbolinas/farmacologia , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos/métodos , Fungicidas Industriais/isolamento & purificação , Fungicidas Industriais/farmacologia , Inseticidas/isolamento & purificação , Inseticidas/farmacologia , Peganum , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Vírus do Mosaico do Tabaco/fisiologia
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