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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 60095Erstellt: 25. Oktober 2026

Pyrazole-4-carboxylic acid → Propane-1-sulfonic acid{2,4-difluoro-3-[5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide

https://huagongshe.com/reaction/60095

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktPyrazole-4-carboxylic acidHCID 3015937—
Edukt1-Propanesulfonamide, N-[3-[(5-bromo-1H-pyrrolo[2,3-b]pyridin-3-yl)carbonyl]-2,4-difluorophenyl]-HCID 11984556—
EduktPropane-1-sulfonic acid{2,4-difluoro-3-[5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amideHCID 49779453—
ProduktPropane-1-sulfonic acid{2,4-difluoro-3-[5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amideHCID 49779453—
Produkt4-{3-[2,6-difluoro-3-(propane-1-sulfonylamino)-benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl)-pyrazole-1-carboxylic acid phenyl esterHCID 53262038—

Reaktionsschritte

Propane-1-sulfonic acid {2,4-difluoro-3-[5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide 23 is prepared according to Scheme 1a, replacing N-[3-(5-bromo-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-2-fluoro-benzenesulfonamide 21 with propane-1-sulfonic acid [3-(5-bromo-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide and replacing 2-methoxy-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyrimidine 22 with 1H-pyrazole-4-carboxylic acid. Propane-1-sulfonic acid {2,4-difluoro-3-[5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide 23 is further reacted according to Scheme 1b to provide 4-{3-[2,6-difluoro-3-(propane-1-sulfonylamino)-benzoyl]-1H-pyrrolo[2,3-b]pyridin-5-yl}-pyrazole-1-carboxylic acid phenyl ester P-1016.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS09440969B2
Quelldatensatzuspto-grants-2016_09
ORD IDord-6a76b275319c4999a36dfe5f892bad66
Quellennotizuspto-grants-2016_09