Synthesis, pharmacological evaluation and molecular docking studies of indanone derivatives

A Method for Synthesis of 3-Hydroxy-1-indanones via Cu-Catalyzed Intramolecular Annulation Reactions

“…To further evaluate the efficiency and potential applications of this reaction, we performed a gram-scale preparation of the product 2a , and we can isolated this product with up to 81% yield (Scheme ). Besides, the transformation of the product 2a to other derivatives was also studied, and the results displayed that compound 2a can be easily converted to 1 H -indene-1,3­(2 H )-dione ( 3 ) through Jones reagent, 2,3-dihydro-1 H -indene-1,3-diol ( 4 ) via NaBH 4 , 3-methoxy-2,2-dimethyl-2,3-dihydro-1 H -inden-1-one ( 5 ) in the presence of NaH/​CH 3 I, and can also form the 2-benzylidene-1 H -indene-1,3­(2 H )-dione ( 6 ) by a two-step operation involving an oxidation and a condensation reaction; indene-1,3-diones showed some important antibacterial, antifungal, and anti-inflammatory activity …”

A Catalyst‐Free, One‐Pot Three‐Component Aminomethylation of α‐Substituted Nitroacetates: Theoretical and Experimental Studies into the Rate‐Accelerating Effects of the Solvent Methanol

“…Column chromatography was performed on silica gel (200–300 mesh) using a mixture of petroleum ether (60–90 °C)/ethyl acetate as eluent. Nitroallylic acetates 1 a ,11c 2 a ,19 isatin‐derived alkenes 4 ,20 6 a ,21 and 9 22 were prepared according to previously reported procedures.…”

Synthesis of 1-indanones with a broad range of biological activity

“…A combination of two or more biologically active moieties may increase or decrease the biological activity. A series of isoxazole fused 1-indanones 64 with increased anti-inflammatory and antimicrobial activity has been synthesized by Giles et al [ 46 ]. In this synthesis, diethyl phthalate ( 61 ) was reacted with ethyl acetate to obtain indane-1,3-dione ( 62 ), followed by a Knoevenagel condensation with a variety aromatic aldehydes to give chalcone derivatives 63 ( Scheme 21 ).…”