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Grant: Discovery Grants Program - Individual

Nipissing University

$24,000.00

Development of synthetic methodologies to access novel fused polycyclic frameworks

EF 2023-24

Résumé
Heterocyclic compounds are one of the most important classes of molecules that are structurally diverse and found ubiquitously in a variety of synthetic drugs, bioactive natural products, pharmaceuticals, agrochemicals and other commercial materials. Among them the indole core, widely regarded as "privileged framework," is a prevalent substructure in many natural products and biologically active compounds. Owing to their special significance, indole-based polycyclic compounds attract special attention as a building block for the development of therapeutic agents by medicinal chemists. A plethora of bioactivities surrounding the indole core continue to be a driving force in the development of new methodology to find useful compounds and increase the heterocyle diversity. Thus, the need for development of efficient and practical syntheses of indoles bearing a variety of substitution patterns is of great significance. The objective of my research program is to explore and develop novel and efficient synthetic methodology of indole-fused polycyclic heterocycles bearing a variety of substitution patterns. To achieve this, I am proposing to exploit the chemistries of transition metal catalysis, substrates having C-C multiple bonds, reactive intermediates and cascade/domino cycloaddition reactions. The long-term goal is to expand my program towards natural product, pharmaceutical agents and unique materials synthesis, while diversifying methodology development aspects to other important heterocycles. The proposed studies will lead to novel indole-based molecular architectures with interesting biological properties and 3-D topologies. These molecules could also further serve as template for synthesizing compounds of desired frameworks following a target based synthesis approach. Particular attention will be given to incorporating green properties (such as, clean and quantitative conversion, mild conditions, catalyst recycling, atom economy, one-pot cascade reactions, and low waste production) to methodologies developed in my laboratory in order to advance their practical and commercial importance. Training of highly qualified personnel will be of utmost importance during this endeavor with a commitment to our values of equity, diversity, and inclusion.
Programme
Discovery Grants Program - Individual
Bénéficiaire
Emplacement
Ontario, Canada
Type de bénéficiaire
Academia
Type
Grant
Source
NSERC's Awards Data

Tel que publié

Application id
RGPIN-2021-03869
Name nom
Jha, Mukund
Department département
Biology - Biology
Organization id
44
Institution établissement
Nipissing University
Province en
Ontario
Province fr
Ontario
Country en
CANADA
Country fr
CANADA
Fiscal year exercice financier
2023
Competition year année de concours
2021
Award amount
24000
Program id
RGPIN
Program name en
Discovery Grants Program - Individual
Program name fr
Programme de subventions à la découverte - individuelles
Group en
DISCOVERY RESEARCH
Group fr
RECHERCHE AXÉE SUR LA DÉCOUVERTE
Committee code
1504
Committee name en
Chemistry
Committee name fr
Chimie
Area of application code
1202
Area of application group en
Advancement of knowledge
Area of application group fr
Avancement des connaissances
Area of application en
Physical sciences
Area of application fr
Sciences physiques
Research subject code
3703
Research subject group en
Organic chemistry
Research subject group fr
Organic syntheses
Research subject en
Chimie organique
Research subject fr
Synthèses organiques
Application title
Development of synthetic methodologies to access novel fused polycyclic frameworks
Keyword
cascade reactions; C-H funactionalization; heterocyclic compounds; hydroamination; hydroarylation; indole; indole-fused; metal-catalyzed; methodology development; S-containing
Application summary
Heterocyclic compounds are one of the most important classes of molecules that are structurally diverse and found ubiquitously in a variety of synthetic drugs, bioactive natural products, pharmaceuticals, agrochemicals and other commercial materials. Among them the indole core, widely regarded as "privileged framework," is a prevalent substructure in many natural products and biologically active compounds. Owing to their special significance, indole-based polycyclic compounds attract special attention as a building block for the development of therapeutic agents by medicinal chemists. A plethora of bioactivities surrounding the indole core continue to be a driving force in the development of new methodology to find useful compounds and increase the heterocyle diversity. Thus, the need for development of efficient and practical syntheses of indoles bearing a variety of substitution patterns is of great significance. The objective of my research program is to explore and develop novel and efficient synthetic methodology of indole-fused polycyclic heterocycles bearing a variety of substitution patterns. To achieve this, I am proposing to exploit the chemistries of transition metal catalysis, substrates having C-C multiple bonds, reactive intermediates and cascade/domino cycloaddition reactions. The long-term goal is to expand my program towards natural product, pharmaceutical agents and unique materials synthesis, while diversifying methodology development aspects to other important heterocycles. The proposed studies will lead to novel indole-based molecular architectures with interesting biological properties and 3-D topologies. These molecules could also further serve as template for synthesizing compounds of desired frameworks following a target based synthesis approach. Particular attention will be given to incorporating green properties (such as, clean and quantitative conversion, mild conditions, catalyst recycling, atom economy, one-pot cascade reactions, and low waste production) to methodologies developed in my laboratory in order to advance their practical and commercial importance. Training of highly qualified personnel will be of utmost importance during this endeavor with a commitment to our values of equity, diversity, and inclusion.