反応 #92272

反応方程式

DIEA

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

CDI

azetidin-3-ol hydrochloride

→

final product

収率 55.0%

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

収率 55.0%

溶媒

DCM

反応条件

後処理

1. 1
   workup.STIRRINGThe reaction was stirred for 30 minutes before it
2. 2
   濃縮was concentrated
3. 3
   その他directly purified by reverse-phase column chromatography
4. 4
   洗浄eluting with 0 to 60% acetonitrile/water

実験手順

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).

出典