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Construction of Bio-active Amino Synthons via Functionalisation of 2-Substituted Azetidines

Implementing Organization

Institute of Chemical Technology
Principal Investigator
Dr. Raju Adepu
Institute of Chemical Technology

About

Small-ring heterocycles are found in a variety of natural products and bio-active compounds. Among them, nitrogen-containing heterocycles have a greater impact due to their extensive pharmacological applications. Aziridine, azetidine, pyrrolidine, etc., are belongs to small size saturated N-heterocycles. The synthetic utility and applications of highly strained three-membered aziridines are well studied in the literature with respect to the opening of the ring via C-N bond cleavage by nucleophiles and various transition metal catalysts due to high strain. The ring strain in four-membered saturated N-heterocycle, azetidines is lies between highly reactive three-membered aziridine and unreacted five-membered pyrrolidine. Due to this, less attention was made towards the ring-opening cross-coupling reactions of four-membered azetidines in comparison to three-membered aziridines to make C-C, C-heteroatom bonds. In this context, the development of deconstructive functionalization of azetidines would be useful in the synthesis of bio-active γ-functionalized alkylamine/amino acid scaffolds. Further substrate-controlled C-H activation of azetidines having bidentate ligand would give the library of densely functionalized and structurally diverse four-membered azetidine ring molecular architectures having significant pharmacological interest.
Funding Organization
Funding Organization
Science and Engineering Research Board (SERB), New Delhi
Anusandhan National Research Foundation (ANRF)
Quick Information
Area of Research
Chemical Sciences
Start Year
2022
End Year
2024
Sanction Amount
₹ 28.24 L
Status
Completed
Output
No. of Research Paper
00
Technologies (If Any)
00
No. of PhD Produced
N/A
Startup (If Any)
00
No. of Patents
Filed :00
Grant :00
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