Recent developments in the synthesis and applications of dihydropyrimidin-2(1H)-ones and thiones

Abstract

Dihydropyrimidin-2(1H)-ones/thiones (DHPMs) are important heterocyclic compounds owing to their excellent biological activities and have been widely utilized in pharmaceutical applications. Recently, numerous DHPM derivatives have been prepared. This review covers the synthesis of DHPMs and improved procedures for the preparation of DHPMs from 1995 to 2016.

1,2,3-Triazole Nucleus as a Versatile Tool for the Obtainment of Novel Biologically Active Compounds: an Overview

“…Vale ressaltar que as dihidropirimidinonas apresentam diferentes atividades biológicas, como: antiprotozoária, antiviral, antifúngica, antibacteriana, anticonvulsivante e outras. [59][60][61][62][63] Tal característica, em conjunto com a baixa citotoxicidade do álcool perílico (17) frente à células saudáveis, 64 pode estimular a realização de futuros ensaios biológicos para avaliar a aplicabilidade dos híbridos 18a-f além do tratamento do câncer. 64 Como último exemplo de hibridação, Oliveira e colaboradores uniram diferentes 4-oxoquinolinas N-alquil substituídas à molécula da naftoquinona (19), sintetizando os híbridos 20a-e a fim de avaliar a atividade combinada anti-Leishmania frente a forma promastigota e amastigota (Tabela 2).…”

Fe(III)/Bentonite as a Heterogeneous Catalyst for the Synthesis of 3,4‐dihydropyrimidin‐2‐(1H)‐ones

“…All mentioned catalysts improved the yield of product but most of them are expensive; difficult to remove from solution consequently metal traces can be remained in the final product and reusability are the key issues. To address these problems, heterogeneous catalysts are extensively employed for this reaction which displayed good activity and reusability and facilitated easy separation of product [28–30] . Various Lewis acids are supported over different kind of solid support for this reaction.…”

Photo-Oxidation Coupled Kabachnik–Fields and Bigenelli Reactions for Direct Conversion of Benzyl alcohols to α-Aminophosphonates and Dihydropyrimidones

“…16 The traditional synthesis of dihydropyrimidones involves use of an aldehyde, a β-keto ester or β-diketone, and urea, 17 with most of the advances involving use of a Brønsted acid 18 or base, 19 metal based Lewis acids, 20 organocatalysts, 21 and heterogeneous catalysts. [22][23][24][25] In this regard, photochemical reactions are undoubtedly greener alternatives to thermal processes, shifting the synthetic path of reaction from its solvo-thermal form to a neat and photochemical form; this has become a major step towards ecofriendly synthetic methodologies. The ap-Ali et al: Photo-Oxidation Coupled Kabachnik-Fields ... plications of photocatalysis have increased significantly in recent times and development of light mediated reactions as sustainable synthetic methodologies is becoming more popular.…”