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New Chemical Process to Selectively Functionalize Pyridines, Diazines and Pharmaceuticals

Award Number: R01GM124094
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: 01/01/2018
PERIOD OF PERFORMANCE END DATE: 06/30/2025

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New Chemical Process to Selectively Functionalize Pyridines, Diazines and Pharmaceuticals - Project Abstract. The goal of this project is to introduce a new synthetic strategy to functionalize pyridine and diazine heterocycles. Pyridines are the second most common nitrogen heterocycle found in FDA approved drugs, and there are numerous examples of diazines in these structures. The widespread occurrence arises because of a combined effect of the heterocycle and its substituents. The key drug-receptor interaction is often comprised of a hydrogen bond between the heterocycles N-lone pairs and the biological target. These heterocycles are also polar, can engage in p-stacking interactions and are resistant to oxidative metabolism. The substituents enable tuning of the steric and electronic environment of the heterocycle as well as serving as additional binding sites. As such, medicinal chemists require chemical process that can directly and selectively install a range of substituents at various stages of drug discovery from C–H precursors. In this proposal we will develop three different approaches for azine functionalization. First, we will install heterocyclic phosphonium salts and exploit their unique reactivity to develop coupling reactions with amines, thiophenols, cysteine containing molecules and alkynes. Using phosphines with pendant functional groups will enable coupling with water and ammonia. Second, direct coupling reactions between NTf-pyridinium salts and nucleophiles will be exploited for C–Heteroatom bond formation. additionsThis platform will enable direct coupling with aliphatic amines, anilines, amides and sulfonamides. Third, we will use sulfur nucleophile to change the regioselectivity of nucleophilic addition from the 4-position of pyridines to the 2-position of the scaffold. Once embedded in the substrate, these sulfur nucleophiles also serve as versatile functional group the enable other transformations to make C–N, C–O and C–F bonds.


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 = -$31,552 )
2025	2024	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	7	4/16/2025	NON-COMPETING CONTINUATION	$0
2025	2024	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	001	7	9/25/2025	NON-COMPETING CONTINUATION	-$31,552
														Subtotal = -$31,552

Issue Date FY: 2024 ( Subtotal = $310,130 )
2024	2024	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	002	7	6/14/2024	NON-COMPETING CONTINUATION	$310,130
2024	2023	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	001	6	3/21/2024	COMPETING CONTINUATION	$32,054
2024	2022	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	5	3/21/2024	NON-COMPETING CONTINUATION	-$32,054
														Subtotal = $310,130

Issue Date FY: 2023 ( Subtotal = $310,178 )
2023	2023	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	001	6	8/7/2023	COMPETING CONTINUATION	$310,178
2023	2022	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	5	7/31/2023	NON-COMPETING CONTINUATION	$0
														Subtotal = $310,178

Issue Date FY: 2022 ( Subtotal = $280,461 )
2022	2022	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	001	5	7/19/2022	NON-COMPETING CONTINUATION	$28,047
2022	2022	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	5	11/23/2021	NON-COMPETING CONTINUATION	$252,414
														Subtotal = $280,461

Issue Date FY: 2021 ( Subtotal = $281,642 )
2021	2021	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	001	4	2/11/2021	NON-COMPETING CONTINUATION	$28,165
2021	2021	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	4	11/10/2020	NON-COMPETING CONTINUATION	$253,477
														Subtotal = $281,642

Issue Date FY: 2020 ( Subtotal = $282,735 )
2020	2020	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	001	3	3/5/2020	NON-COMPETING CONTINUATION	$28,274
2020	2020	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	3	12/13/2019	NON-COMPETING CONTINUATION	$254,461
														Subtotal = $282,735

Issue Date FY: 2019 ( Subtotal = $283,747 )
2019	2019	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	2	12/11/2018	NON-COMPETING CONTINUATION	$283,747
														Subtotal = $283,747

Issue Date FY: 2018 ( Subtotal = $284,684 )
2018	2018	COLORADO STATE UNIVERSITY	601 S HOWES ST	FORT COLLINS	CO	80521	LARIMER	USA	Biomedical Research and Research Training	000	1	12/6/2017	NEW	$284,684
														Subtotal = $284,684

Grand Total All Awards = $2,002,025

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New Chemical Process to Selectively Functionalize Pyridines, Diazines and Pharmaceuticals

Award Number: R01GM124094

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: 01/01/2018

PERIOD OF PERFORMANCE END DATE: 06/30/2025

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