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HRID 536319Erstellt: 24. Oktober 2026

Pyridine → 3,5-Dimethyl-isoxazole-4-carboxylic acid [2-methyl-6-((2S,3'R)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-pyridin-3-yl]-amide

https://huagongshe.com/de/reaction/536319

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktPyridineHCID 1049—
EduktTris(hydroxymethyl)aminomethaneHCID 6503—
Edukt3,5-Dimethylisoxazole-4-carbonyl ChlorideHCID 2736265—
Edukt2-methyl-6-[(3R)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-amineHCID 67480461—
Lösungsmittel1,2-DichloroethaneHCID 11—
Produkt3,5-Dimethyl-isoxazole-4-carboxylic acid [2-methyl-6-((2S,3'R)-2-methyl-[1,3']bipyrrolidinyl-1'-yl)-pyridin-3-yl]-amideHCID 5459715635,9%

Reaktionsschritte

To a solution of 2-methyl-6-[(3R)-3-[(2S)-2-methylpyrrolidin-1-yl]pyrrolidin-1-yl]pyridin-3-amine (22.7 mg, 0.09 mmol) in DCE (1 mL) was added pyridine (0.22 mL, 2.7 mmol) followed by a solution of 3,5-dimethyl-isoxazole-4-carbonyl chloride (43 mg, 0.27 mmol) in DCE (1 mL) and stirred at ambient temperature for 5 hours. To this mixture was then added trisamine resin (200 mg, 0.8 mmol, 4 mmol/g loading), stirred for 30 min, filtered and concentrated to afford a crude solid which was purified by flash column chromatography (5% 7N NH3 in MeOH/CH2Cl2) to obtain 12.4 mg of the title compound.

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08859588B2
Quelldatensatzuspto-grants-2014_10
ORD IDord-df017cd31ca74dc7a4ea446d02557373
Quellennotizuspto-grants-2014_10