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Catalytic and Stereoselective C-C-Heteroatom Bond Forming Reactions

Award Number: R35GM128695
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: 07/15/2018
PERIOD OF PERFORMANCE END DATE: 06/30/2028

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Catalytic and Stereoselective C-C-Heteroatom Bond Forming Reactions - Strategies to access desirable analogues of natural products and pharmaceuticals in efficient, practical, cost-effective, and stereoselective manners are central to organic synthesis and drug discovery. Total synthesis of such analogues is often lengthy and inefficient, thus increasing the time required to secure the desired molecules, as well as the cost of preparing compounds that are important to human healthcare. Particularly attractive but challenging are schemes that enable direct transformation of ubiquitous but otherwise chemically inert C–H bonds that are contained in the polyfunctional bioactive molecules. We will develop catalytic processes that entail oxidation of amine, ether, or thioether-based small molecule drugs into the corresponding enamine, enol ether or thioenol ether derivatives; such intermediates will then be coupled with various chemical tagging agents to generate – in a single operation – a library of drug derivatives. The resulting compounds will contain ‘clickable’ handles that can be used as a handle for bioconjugation. Some will carry tags for structure-activity relationship studies (e.g., biotin, fluorophore), and/or photoaffinity labels for chemoproteomics (e.g., arylazide, diazirine). Various desirable analogues of N, O, and/or S-based medicinal agents will thus become readily accessible; preparation of these entities by total synthesis would either be impossible or substantially more cumbersome. A combination of Lewis acid and Brønsted base catalysts will be used to promote the proposed transformations. We will utilize the above strategies to design pathways that are significantly more efficient and broadly applicable than those previously disclosed. Among the medicinally relevant molecules that will be subjected to the late-stage functionalization are important anticancer agents such as alectinib, carfilzomib, and venetoclax.


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: 2025 ( Subtotal = $483,000 )
2025	2025	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Biomedical Research and Research Training	001	8	6/2/2025	NON-COMPETING CONTINUATION	$483,000
2025	2024	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Biomedical Research and Research Training	000	7	11/6/2024	NON-COMPETING CONTINUATION	$0
														Subtotal = $483,000

Issue Date FY: 2024 ( Subtotal = $483,000 )
2024	2024	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Biomedical Research and Research Training	002	7	6/18/2024	NON-COMPETING CONTINUATION	$483,000
2024	2023	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Biomedical Research and Research Training	001	6	6/5/2024	COMPETING CONTINUATION	$189,200
2024	2022	TRUSTEES OF BOSTON COLLEGE	140 COMMONWEALTH AVE	CHESTNUT HILL	MA	02467	MIDDLESEX	USA	Biomedical Research and Research Training	000	5	6/5/2024	NON-COMPETING CONTINUATION	-$189,200
														Subtotal = $483,000

Issue Date FY: 2023 ( Subtotal = $457,045 )
2023	2023	UNIVERSITY OF FLORIDA	1523 UNION RD RM 207	GAINESVILLE	FL	32611	ALACHUA	USA	Biomedical Research and Research Training	000	6	6/22/2023	COMPETING CONTINUATION	$457,045
														Subtotal = $457,045

Issue Date FY: 2022 ( Subtotal = $391,250 )
2022	2022	TRUSTEES OF BOSTON COLLEGE	140 COMMONWEALTH AVE	CHESTNUT HILL	MA	02467	MIDDLESEX	USA	Biomedical Research and Research Training	000	5	9/6/2022	NON-COMPETING CONTINUATION	$391,250
														Subtotal = $391,250

Issue Date FY: 2021 ( Subtotal = $391,250 )
2021	2021	TRUSTEES OF BOSTON COLLEGE	140 COMMONWEALTH AVE	CHESTNUT HILL	MA	02467	MIDDLESEX	USA	Biomedical Research and Research Training	000	4	6/8/2021	NON-COMPETING CONTINUATION	$391,250
														Subtotal = $391,250

Issue Date FY: 2020 ( Subtotal = $389,338 )
2020	2020	TRUSTEES OF BOSTON COLLEGE	140 COMMONWEALTH AVE	CHESTNUT HILL	MA	02467	MIDDLESEX	USA	Biomedical Research and Research Training	000	3	6/2/2020	NON-COMPETING CONTINUATION	$389,338
														Subtotal = $389,338

Issue Date FY: 2019 ( Subtotal = $370,176 )
2019	2019	BOSTON COLLEGE, TRUSTEES OF	140 COMMONWEALTH AVE	CHESTNUT HILL	MA	02467	MIDDLESEX	USA	Biomedical Research and Research Training	000	2	7/3/2019	NON-COMPETING CONTINUATION	$370,176
														Subtotal = $370,176

Issue Date FY: 2018 ( Subtotal = $382,514 )
2018	2018	BOSTON COLLEGE, TRUSTEES OF	140 COMMONWEALTH AVE	CHESTNUT HILL	MA	02467	MIDDLESEX	USA	Biomedical Research and Research Training	000	1	7/4/2018	NEW	$382,514
														Subtotal = $382,514

Grand Total All Awards = $3,347,573

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Catalytic and Stereoselective C-C-Heteroatom Bond Forming Reactions

Award Number: R35GM128695

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: 07/15/2018

PERIOD OF PERFORMANCE END DATE: 06/30/2028

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