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Iodine/hypervalent iodine mediated intramolecular dehydrogenative cyclisation for synthesis of natural product and pharmaceutically important motifs

Implementing Organization

Goa University
Principal Investigator
Dr. Prajesh Sitaram Volvoikar
Goa University

About

Aim of synthetic chemist is to synthesize a target molecule is most efficient and effective ways which could be ultimately scaled up for commercial use. Cross dehydrogenative coupling (CDC) has gained tremendous importance is last two decades which have given access to vast and varied type of substrates. The process involved in these CDC reactions are often without pre-functionalization of substrates which is cost beneficial. Although tremendous methods of these CDC reaction are available, the applications of these methodologies for synthesis of natural products and for intramolecular cyclisation are very less explored. Also, many studies are on metal catalyst which often results in final products contamination with metal traces, removal of which could to difficult and time consuming. Here in we propose the use of iodine or hypervalent iodine in presence of suitable oxidant on substrates which contains electrophile and nucleophile unit in one molecule. This substrates under reaction conditions will provide either natural products and its derivatives or synthetically important substrates. The conditions for cyclisation will vary from one substrate to another, which will be carefully screened and applied for synthesis of natural products, and to generate library of compounds for testing of biological activity. The intramolecular dehydrogenative cyclisation (IDC) will be used for synthesis of substituted N-methyl-2 alkyl -3-acetyl indoles, cyclisation of substituted N,N-dimethyl[1,1'-biphenyl]-2-amine for synthesis of naturally occurring dihydrobicolorine, trisphaeridine and its derivatives. Also, IDC will be applied for synthesis of calothrixin A, calothrixin B, tryptanthrin, nuevamine and its derivatives which are known for its potent biological activities. This method will definitely be low cost, environment friendly and efficient in synthesizing some of these pharmaceutically important core and natural products.
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
₹ 33.00 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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