Thursday, May 8, 2025 5/8/2025

Ligand-promoted Enantioselective C-H Activation Reactions

Award Number: R01GM084019
ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

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Ligand-promoted Enantioselective C-H Activation Reactions - Project Summary Desymmetrizing activation of prochiral C–H bonds via metal insertion has emerged as a potentially transformative approach for the rapid and divergent synthesis of chiral compounds. However, a significant challenge prohibiting the broad utility of this approach is the poor reactivity of native substrates in the absence of externally-appended directing groups. This proposal directly addresses this challenge by developing two approaches to achieve the enantioselective C–H activation of a range of native substrates commonly found in organic synthesis and drug discovery—carboxylic acids, ketones, aldehydes and amines: (A) Development of chiral bidentate L,X-type ligands containing N-acetyl or pyridone motifs to accelerate C–H cleavage; (B) Development of chiral transient directing groups (TDGs) to enable enantioselective C–H activation of ketones, aldehydes and amines. Following initial discoveries of chiral ligands and TDGs, we will then develop various catalytic cycles to enable the enantioselective C–H activation of diverse native substrates, forming a range of carbon–carbon and carbon–heteroatom bonds asymmetrically. These novel reactions will provide a versatile platform for the construction of -, -, and -stereocenters. These technologies will be applied to drug discovery in collaboration with the pharmaceutical industry and academic laboratories. Specifically, the one- step access to the atypical chiral -lactones and lactams via enantioselective C–H activation will be applied to the discovery of covalent inhibitors for serine hydrolases and cysteine-dependent proteins using activity-based protein profiling.


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: 2024 ( Subtotal = $851,459 )
2024	2024	SCRIPPS RESEARCH INSTITUTE	10550 N TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	17	7/16/2024	NON-COMPETING CONTINUATION	$607,233
2024	2024	SCRIPPS RESEARCH INSTITUTE	10550 N TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	002	17	9/9/2024	SUPPLEMENT FOR EXPANSION	$244,226
2024	2023	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	16	10/11/2023	NON-COMPETING CONTINUATION	$0
														Subtotal = $851,459

Issue Date FY: 2023 ( Subtotal = $706,879 )
2023	2023	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	16	6/27/2023	NON-COMPETING CONTINUATION	$597,333
2023	2023	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	15	5/24/2023	SUPPLEMENT FOR EXPANSION	$109,546
														Subtotal = $706,879

Issue Date FY: 2022 ( Subtotal = $585,782 )
2022	2022	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	15	6/22/2022	NON-COMPETING CONTINUATION	$585,782
														Subtotal = $585,782

Issue Date FY: 2021 ( Subtotal = $585,782 )
2021	2021	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	002	14	9/5/2021	COMPETING CONTINUATION	$7,957
2021	2021	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	14	6/28/2021	COMPETING CONTINUATION	$585,782
2021	2020	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	13	9/5/2021	NON-COMPETING CONTINUATION	-$7,957
														Subtotal = $585,782

Issue Date FY: 2020 ( Subtotal = $619,200 )
2020	2020	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	13	6/12/2020	NON-COMPETING CONTINUATION	$619,200
														Subtotal = $619,200

Issue Date FY: 2019 ( Subtotal = $766,613 )
2019	2019	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	12	8/7/2019	NON-COMPETING CONTINUATION	$619,200
2019	2019	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	12	8/8/2019	SUPPLEMENT FOR EXPANSION	$147,413
														Subtotal = $766,613

Issue Date FY: 2018 ( Subtotal = $619,200 )
2018	2018	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	002	11	6/25/2018	NON-COMPETING CONTINUATION	$619,200
2018	2017	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	10	12/2/2017	COMPETING CONTINUATION	$7,957
2018	2016	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	9	12/2/2017	SUPPLEMENT FOR EXPANSION	-$7,957
														Subtotal = $619,200

Issue Date FY: 2017 ( Subtotal = $619,200 )
2017	2017	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	10	5/8/2017	COMPETING CONTINUATION	$619,200
2017	2015	SCRIPPS RESEARCH INSTITUTE, THE	10550 NORTH TORREY PINES RD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	8	10/26/2016	NON-COMPETING CONTINUATION	$0
														Subtotal = $619,200

Issue Date FY: 2016 ( Subtotal = $680,321 )
2016	2016	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	9	6/16/2016	EXTENSION WITH OR WITHOUT FUNDS	$539,000
2016	2016	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	001	9	9/7/2016	SUPPLEMENT FOR EXPANSION	$141,321
														Subtotal = $680,321

Issue Date FY: 2015 ( Subtotal = $530,600 )
2015	2015	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	8	6/19/2015	NON-COMPETING CONTINUATION	$530,600
														Subtotal = $530,600

Issue Date FY: 2014 ( Subtotal = $530,600 )
2014	2014	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	7	7/29/2014	NON-COMPETING CONTINUATION	$530,600
														Subtotal = $530,600

Issue Date FY: 2013 ( Subtotal = $530,600 )
2013	2013	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	6	6/28/2013	COMPETING CONTINUATION	$530,600
														Subtotal = $530,600

Issue Date FY: 2012 ( Subtotal = $371,458 )
2012	2012	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	5	5/18/2012	NON-COMPETING CONTINUATION	$371,458
														Subtotal = $371,458

Issue Date FY: 2011 ( Subtotal = $371,458 )
2011	2011	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	4	5/23/2011	NON-COMPETING CONTINUATION	$371,458
														Subtotal = $371,458

Issue Date FY: 2010 ( Subtotal = $375,210 )
2010	2010	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	3	5/13/2010	NON-COMPETING CONTINUATION	$375,210
														Subtotal = $375,210

Issue Date FY: 2009 ( Subtotal = $379,000 )
2009	2009	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	2	5/26/2009	NON-COMPETING CONTINUATION	$379,000
														Subtotal = $379,000

Issue Date FY: 2008 ( Subtotal = $379,000 )
2008	2008	SCRIPPS RESEARCH INSTITUTE	10666 NORTH TORREY PINES ROAD	LA JOLLA	CA	92037	SAN DIEGO	USA	Biomedical Research and Research Training	000	1	7/21/2008	NEW	$379,000
														Subtotal = $379,000

Grand Total All Awards = $9,502,362

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Ligand-promoted Enantioselective C-H Activation Reactions

Award Number: R01GM084019

ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

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

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