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HRID 249817作成日:2026年10月27日

Hydrochloric Acid → {2,4-difluoro-3-[hydroxy-(1H-pyrrolo[2,3-b]pyridin-3-yl)-methyl]-phenyl}-carbamic acid benzyl ester

https://huagongshe.com/reaction/249817

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrochloric AcidHCID 313—
反応物MethanolHCID 887—
反応物Potassium HydroxideHCID 14797—
反応物5-Chloro-1H-pyrrolo[2,3-b]pyridineHCID 24229213—
反応物Benzyl (2,4-difluoro-3-formylphenyl)carbamateHCID 58086235—
生成物{2,4-difluoro-3-[hydroxy-(1H-pyrrolo[2,3-b]pyridin-3-yl)-methyl]-phenyl}-carbamic acid benzyl esterHCID 6667927850.6%

反応手順

Into a round bottom flask was added 5-chloro-1-pyrrolo[2,3-b]pyridine (6, 0.524 g, 3.43 mmol, prepared as described in Example 5) in methanol (5.00 mL, 0.123 mol). Potassium hydroxide (0.800 g, 14.2 mmol) and (2,4-difluoro-3-formyl-phenyl)-carbamic acid benzyl ester (53, 1.02 g, 3.5 mmol) were added and the reaction mixture was stirred overnight. The reaction mixture was poured into 1N HCl and extracted with ethyl acetate. The organic layer was washed with brine, dried over sodium sulfate, concentrated and crystallized from ethyl acetate to give compound 54 (710 mg, 46%). MS (ESI)[M+H+]+=444.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07863289B2
出典データセットuspto-grants-2011_01
ORD IDord-597c4724684e4fcfb69cb29bb8609a82
出典メモuspto-grants-2011_01