تفاعل #92272

معادلة التفاعل

DIEA

5-(2-(3-fluorophenyl)-2-methylpyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-amine

CDI

azetidin-3-ol hydrochloride

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final product

المردود 55.0%

N-(5-(2-(3-fluorophenyl)-2-methylpyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxyazetidine-1-carboxamide

المردود 55.0%

المذيبات

DCM

ظروف التفاعل

المعالجة

1. 1
   workup.STIRRINGThe reaction was stirred for 30 minutes before it
2. 2
   تركيزwas concentrated
3. 3
   أخرىdirectly purified by reverse-phase column chromatography
4. 4
   غسيلeluting with 0 to 60% acetonitrile/water

الإجراء التجريبي

To a DCM (0.7 mL) solution of 5-(2-(3-fluorophenyl)-2-methylpyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-amine (25 mg, 0.08 mmol) was added CDI (20 mg, 0.12 mmol) at ambient temperature in one portion. After stirring one hour, azetidin-3-ol hydrochloride (20 mg, 0.12 mmol) was added in one portion, followed by addition of DIEA (0.028 mL, 0.16 mmol). The reaction was stirred for 30 minutes before it was concentrated and directly purified by reverse-phase column chromatography, eluting with 0 to 60% acetonitrile/water to yield the final product as a yellowish oil (18 mg, 55% yield). MS (apci) m/z=411.2 (M+H).

المصدر