# Synthesis of Bioactive Small Molecule Building Blocks

> **NIH NIH R35** · UNIV OF NORTH CAROLINA CHAPEL HILL · 2022 · $460,679

## Abstract

Project Summary
A significant obstacle to the creation of the next generation of small molecule therapeutics is the lack of general
and efficient methods for accessing certain stereochemically dense structures that contain functionality
important for bioactivity. This application seeks to continue a productive MIRA program concerned with the
laboratory preparation of chiral, functionalized bioactive small molecule building blocks. The general goal of
this program is to develop new synthetic chemistry platforms that will enable the rapid and selective
construction of new structures of immediate relevance for biomedical applications.
Key challenges that we seek to address in the coming project period include:
 • Enantioconvergent reactions: A significant expansion of general strategies and reaction platforms that
 catalytically convert readily accessible racemic starting materials into high value, enantiomerically
 enriched products;
 • Salt-based catalysis: The development of broad new catalysis modes that operate by quasi-
 intramolecular mechanisms enabled by ionic tethering;
 • Dearomatization of feedstock arenes: The development of useful oxidative dearomatization reactions
 that convert readily available aromatic building blocks into functionalized enantiomerically pure building
blocks;
 • Natural product synthesis: The efficient synthesis and biological evaluation of complex natural products
 and new structural analogs.
Collectively, we expect that these MIRA research activities will provide facile access to structures that were
heretofore unknown or accessible only by virtue of methods that were inefficient and/or impractical. The
program generates new chemical knowledge in the form of new reactions and catalysts for use by the scientific
community, and also provides new chemical matter for us to study with our biological collaborators on problems
of biomedical relevance.

## Key facts

- **NIH application ID:** 10380693
- **Project number:** 5R35GM118055-07
- **Recipient organization:** UNIV OF NORTH CAROLINA CHAPEL HILL
- **Principal Investigator:** Jeffrey S Johnson
- **Activity code:** R35 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2022
- **Award amount:** $460,679
- **Award type:** 5
- **Project period:** 2016-05-01 → 2026-04-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10380693

## Citation

> US National Institutes of Health, RePORTER application 10380693, Synthesis of Bioactive Small Molecule Building Blocks (5R35GM118055-07). Retrieved via AI Analytics 2026-05-21 from https://api.ai-analytics.org/grant/nih/10380693. Licensed CC0.

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