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Novel Bowl-shaped Catalysts for Selective C-H Functionalization

Award Number: R35GM158221
ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 08/01/2025
PERIOD OF PERFORMANCE END DATE: 05/31/2030

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Novel Bowl-shaped Catalysts for Selective C-H Functionalization - 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. Particularly important in the current era is the development of new strategies to access chiral scaffolds as it is generally recognized that there are has been an overreliance on the use of planar scaffolds for drug candidates. Enantioselective C-H functionalization is the central focus of this proposal. It represents an exciting new approach but a major challenge has been how to control site-selectivity in substrates containing multiple C-H bonds. The Davies group pioneered the rhodium-catalyzed chemistry of donor/acceptor carbene intermediates and found that these carbenes are exceptionally effective as selective C-H functionalization. In order to maximize their synthetic potential, Davies designed chiral catalysts of different shapes and sizes to control the three dimensional shape of the products and which C-H bond will be functionalized. His first generation catalyst was effective at reacting at activated C-H bonds. His second generation catalysts were sterically demanding and could distinguish between primary, secondary and tertiary C-H bonds at unactivated site. The third generation catalysts described in this proposal are bowl-shaped catalysts and are capable of subtle site selectivity between very similar C-H bonds. The secondary structure of the bowl plays a critical role in the selectivity. The program over the next five years will evaluate four series of bowl-shaped catalysts with a range of challenging substrates. In addition, the systems will be optimized so that it can operate under extremely low catalyst loadings. Many of the targets are related to compounds of pharmaceutical interest and the Davies group will work closely with companies to ensure the new methodology is impactful in drug discovery and large scale process chemistry.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2026 ( Subtotal = $371,304 )
2026	2026	EMORY UNIVERSITY	201 DOWMAN DR NE	ATLANTA	GA	30322	DEKALB	USA	Biomedical Research and Research Training	000	2	5/12/2026	NON-COMPETING CONTINUATION	$371,304
														Subtotal = $371,304

Issue Date FY: 2025 ( Subtotal = $373,117 )
2025	2025	EMORY UNIVERSITY	201 DOWMAN DR NE	ATLANTA	GA	30322	DEKALB	USA	Biomedical Research and Research Training	000	1	7/14/2025	NEW	$373,117
														Subtotal = $373,117

Grand Total All Awards = $744,421

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Novel Bowl-shaped Catalysts for Selective C-H Functionalization

Award Number: R35GM158221

ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 08/01/2025

PERIOD OF PERFORMANCE END DATE: 05/31/2030

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