Simultaneous ultrasound- and microwave-assisted one-pot ‘click’ synthesis of 3-formyl-indole clubbed 1,2,3-triazole derivatives and their biological evaluation was written by Mokariya, Jaydeep A.;Kalola, Anirudhdha G.;Prasad, Pratibha;Patel, Manish P.. And the article was included in Molecular Diversity in 2022.Recommanded Product: Ethyl 4-chloro-3-oxobutanoate The following contents are mentioned in the article:
An environment friendly, high yielding, promising one-pot protocol for the click reaction of N-propargyl-3-formylindoles, chloroacetic acid/ester and sodium azide, leading to the formation of 3-formyl-indole clubbed 1,4-disubstituted-1,2,3-triazole derivatives I [R = OH, OEt, Ph, etc.; R1 = H, Me] aided by CuI catalyst accomplished under acceleration of simultaneous ultrasound and microwave irradiation in a very short reaction time was described. Further, acid derivatives I [R = OH; R1 = H, Me] were subjected to acid-amine coupling reaction with secondary amines in the presence of HATU to afford triazoles II [R2 = 4-methylpiperidin-1-yl, 2-morpholino, 1,2,3-triazol-1-yl, etc.]. The perspective of this protocol was to get rid of the hectic preparation and handling of organic azide which are generated in situ. Consequently, this protocol blossomed the click process by making it environment benign, user-friendly, safe and clean technique. All the synthesized compounds were preliminarily screened for their in vitro antimicrobial activity against a panel of pathogenic strains. The majority of compounds possessed noticeably inhibitory action against E. Coli, S. Typhi, P. Aeruginosa, C. tetani, S. aureus and B. subtillis. Among all compounds, I [R1 = H, R2 = 4-methylpiperidin-1-yl; R1 = Me, R2 = 4-methylpiperazin-1-yl] exhibited excellent inhibitory action against E.Coli and P. Aeruginosa strain, resp., as compared to standard drug. One compound I [R = Me, R1 = OEt] showed remarkable potency against fungal strain. Mol. docking study was carried out to understand binding of compound with protein. In silico ADME prediction was carried out to check physicochem. properties of synthesized compound This study involved multiple reactions and reactants, such as Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3Recommanded Product: Ethyl 4-chloro-3-oxobutanoate).
Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Recommanded Product: Ethyl 4-chloro-3-oxobutanoate
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics