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HRID 875681作成日:2026年10月26日

(3R)-3-Aminopiperidine, 3-BOC protected → (R)-tert-butyl 1-(5-bromo-3-(3-methylbenzamido)-1H-pyrrolo[2,3-b]pyridin-4-yl)piperidin-3-ylcarbamate

https://huagongshe.com/reaction/875681

反応式

関与物質

役割名称HCID仕込み量
反応物(3R)-3-Aminopiperidine, 3-BOC protectedHCID 1514172—
反応物N-(5-bromo-4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-3-methylbenzamideHCID 60205331—
溶媒1-ButanolHCID 263—
生成物(R)-tert-butyl 1-(5-bromo-3-(3-methylbenzamido)-1H-pyrrolo[2,3-b]pyridin-4-yl)piperidin-3-ylcarbamateHCID 6704539047.3%

反応手順

N-(5-Bromo-4-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)-3-methylbenzamide (210 mg, 0.60 mmol) and (R)-tert-butyl piperidin-3-ylcarbamate (360 mg, 1.8 mmol) in n-BuOH (3 mL) was stirred at 155° C. in a sealed tube. The reaction was then cooled to room temperature and concentrated to dryness. The crude residue was purified by reverse phase HPLC to give (R)-tert-butyl 1-(5-bromo-3-(3-methylbenzamido)-1H-pyrrolo[2,3-b]pyridin-4-yl)piperidin-3-ylcarbamate (150 mg, 47% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08981085B2
出典データセットuspto-grants-2015_03
ORD IDord-34aa1e2a24bd49bca1f35b572e8596fe
出典メモuspto-grants-2015_03