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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 536528생성일: 2026년 10월 27일

Water → 4-(4,4-Difluoropiperidin-1-yl)-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5,5-dimethyl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one

https://huagongshe.com/reaction/536528

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참여 물질

역할이름HCID투입량
반응물WaterHCID 962—
반응물DiisopropylethylamineHCID 81531—
반응물4,4-Difluoropiperidine hydrochlorideHCID 2758351—
반응물2-[5-Fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-iodo-5,5-dimethyl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-oneHCID 86705366—
용매N-methyl-2-pyrrolidoneHCID 13387—
생성물4-(4,4-Difluoropiperidin-1-yl)-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5,5-dimethyl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-oneHCID 7129029266.6%

반응 조건

온도150 °C

반응 단계

100 mg (0.18 mmol) of 2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-4-iodo-5,5-dimethyl-5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one (example 16A) was dissolved in 1-methyl-2-pyrrolidone (3.1 ml) in a reaction vessel suitable for a microwave, and 0.19 ml (1.07 mmol) of N,N-diisopropyl ethylamine and 140 mg (0.89 mmol) of 4,4-difluoropiperidine hydrochloride were added. Then the reaction vessel was sealed with a septum and was heated in the microwave for 5 h at 150° C. Then the same amounts of N,N-diisopropyl ethylamine and 4,4-difluoropiperidine hydrochloride were added again to the reaction solution and the reaction mixture was stirred for 6 h at 150° C. in the microwave. Water was added to the reaction mixture, the precipitated solid was stirred for 30 min at room temperature and then filtered off. The precipitated solid was stirred with 1 ml acetonitrile, the solid was filtered off and was washed with 0.5 ml acetonitrile. 63 mg of the target compound (64% of theor.) was obtained.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08859569B2
출처 데이터셋uspto-grants-2014_10
ORD IDord-63efb829cd884fab97ccb883ec81241a
출처 메모uspto-grants-2014_10