# New Methods and Strategies for the Concise Synthesis of Bioactive Polycyclic Molecules

> **NIH NIH R01** · NORTHWESTERN UNIVERSITY · 2021 · $288,681

## Abstract

Project Summary
 The discovery and development of effective chemical therapeutics for human disease is limited by the
shortcomings of synthetic chemistry that make investigating important chemical structures difficult. In
particular, the clinical potential of many complex polycyclic structures is under-explored due to a lack of
methods for their preparation. Bridging this gap will allow many new structures to be synthesized rapidly,
leading to an increased rate at which new therapeutics are discovered.
 The long-term goal of this research program is to make significant contributions to both chemistry and
medicine by developing general synthetic strategies for the rapid preparation of biologically active complex
polycyclic structures. The specific goals of the proposed research are to establish new strategies for the rapid
and stereocontrolled synthesis of a diverse range of pharmacologically relevant polycyclic small-molecules,
including natural products and synthetic natural product-like scaffolds. Our research is focused by two specific
aims that seek to provide access to unique and challenging chemotypes through efficient and modular
fragment coupling processes.
 The Specific Aims of the project are: 1. Develop Unified Strategies to Access Stereochemically Challenging
Chemotypes – In this Aim oxidative coupling of simple enone substrates is a central methodological focus. 2.
Develop Catalytic Fragment Couplings for Accessing Diverse Ring Systems – in this Aim a series of new
BrØnsted acid catalyzed reactions are put forth.
 The proposed research is innovative because it will utilize general reactions to access a wide range of
challenging molecules with different structures from readily prepared and structurally simple building blocks.
The expected outcomes of this research will be the concise synthesis of many medicinally important structures
that are challenging to current methods. This proposed research is significant for human health because it is
expected to provide underexplored complex polycyclic structures in quantities that will ensure their utilization in
discovering new chemical therapeutics.

## Key facts

- **NIH application ID:** 10104516
- **Project number:** 5R01GM124089-04
- **Recipient organization:** NORTHWESTERN UNIVERSITY
- **Principal Investigator:** Regan James Thomson
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $288,681
- **Award type:** 5
- **Project period:** 2018-05-01 → 2024-02-29

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10104516

## Citation

> US National Institutes of Health, RePORTER application 10104516, New Methods and Strategies for the Concise Synthesis of Bioactive Polycyclic Molecules (5R01GM124089-04). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10104516. Licensed CC0.

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