# New Directions in Enantioselective C-H Functionalization

> **NIH NIH R01** · EMORY UNIVERSITY · 2020 · $356,753

## Abstract

Project Summary
The development of new synthetic methods has the potential to transform how pharmaceutical
drugs are made and even what types of compounds will be designed as potential targets. The
synthetic accessibility is a crucial component in the design of drugs and entirely new synthetic
strategies open up new vistas of potential targets for consideration. A transformation that has
generated considerable recent interest is C-H functionalization, because it represents a different
logic for how to join molecules together. One of the major challenges is to control the site
selectivity in substrates containing multiple C-H bonds. A promising approach has been the
rhodium-catalyzed reactions of donor/acceptor carbenes, which by using the right catalyst, will
allow selective reactions to occur at either primary, secondary of tertiary C-H bonds. A major,
limitation associated with this approach, however, is the narrow range of donor/acceptor carbenes
that are currently used, primarily limited to carbenes derived from vinyl- aryl- and
heteroaryldiazoacetates.
This proposal focuses on the development of new types of donor/acceptor carbenes, which will
greatly enhance the synthetic versatility of this promising methodology to access new chemical
space. This will be achieved by expanding the range of functionality that can be associated with
the donor/acceptor carbene chemistry, designing a new class of high symmetry bowl-shaped
chiral catalysts, and illustrating new strategic opportunities for catalyst-controlled C-H
functionalization applied to pharmaceutically relevant targets.

## Key facts

- **NIH application ID:** 10121603
- **Project number:** 2R01GM099142-09
- **Recipient organization:** EMORY UNIVERSITY
- **Principal Investigator:** HUW M DAVIES
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $356,753
- **Award type:** 2
- **Project period:** 2011-09-20 → 2024-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10121603

## Citation

> US National Institutes of Health, RePORTER application 10121603, New Directions in Enantioselective C-H Functionalization (2R01GM099142-09). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/10121603. Licensed CC0.

---

*[NIH grants dataset](/datasets/nih-grants) · CC0 1.0*