Cinchonine-driven multi-component domino Knoevenagel–Michael strategy: metal-free synthesis of quinoline-based 4H-pyran and tetrahydro-4H-chromene derivatives

Research on Chemical Intermediates - Cinchonine-catalyzed simple, expeditious, and efficient protocol for the synthesis of quinoline-based 4H-pyran and tetrahydro-4H-chromenes has been demonstrated...     

CeCl3⋅7H2O-catalysed hydrophosphonylation of aldehydes and ketones: An expeditious route to α-hydroxyphosphonates under solvent-free conditions

Abstract

A cerium(III) chloride-catalysed expeditious synthesis of α-hydroxyphosphonates via a modified Abramov synthetic protocol has been developed. The scope of the current protocol is broad, with a range of aromatic, α,β-unsaturated and heterocyclic aldehydes being efficiently converted to the anticipated products in very good to excellent yields (89–96%) in 15?min using low catalytic loading. The protocol was efficiently extended to hitherto unactivated cyclic ketones such as cyclopentanone and cyclohexanone to afford the required products in excellent yields. However, the reaction with cyclohexenone delivered a Michael product instead of the anticipated α-hydroxyphosphonates. The solvent-free conditions, low catalytic loadings, avoidance of toxic reagents and good to excellent yields are significant advantages of this protocol.     

LiBr-catalyzed one-pot three-component domino strategy toward the construction of β-phosphonomalonates scaffolds in aqueous conditions

Abstract

LiBr-mediated domino Knoevenagel-phospha-Michael strategy has been established for the synthesis of β-phosphonomalonates under aqueous conditions. It is noteworthy that the developed protocol is effective with a wide range of aldehydes to deliver a diverse range of β-phosphonomalonates in good to excellent yields. The mild reaction conditions, easier procedure, use of aqueous media, inexpensive and water tolerant property of LiBr are important advantages of this protocol.     

Rediscovering the Therapeutic Potential of Agarwood in the Management of Chronic Inflammatory Diseases

The inflammatory response is a central aspect of the human immune system that acts as a defense mechanism to protect the body against infections and injuries. A dysregulated inflammatory response is a major health concern, as it can disrupt homeostasis and lead to a plethora of chronic inflammatory conditions. These chronic inflammatory diseases are one of the major causes of morbidity and mortality worldwide and the need for them to be managed in the long term has become a crucial task to alleviate symptoms and improve patients’ overall quality of life. Although various synthetic anti-inflammatory agents have been developed to date, these medications are associated with several adverse effects that have led to poor therapeutic outcomes. The hunt for novel alternatives to modulate underlying chronic inflammatory processes has unveiled nature to be a plentiful source. One such example is agarwood, which is a valuable resinous wood from the trees of Aquilaria spp. Agarwood has been widely utilized for medicinal purposes since ancient times due to its ability to relieve pain, asthmatic symptoms, and arrest vomiting. In terms of inflammation, the major constituent of agarwood, agarwood oil, has been shown to possess multiple bioactive compounds that can regulate molecular mechanisms of chronic inflammation, thereby producing a multitude of pharmacological functions for treating various inflammatory disorders. As such, agarwood oil presents great potential to be developed as a novel anti-inflammatory therapeutic to overcome the drawbacks of existing therapies and improve treatment outcomes. In this review, we have summarized the current literature on agarwood and its bioactive components and have highlighted the potential roles of agarwood oil in treating various chronic inflammatory diseases.