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HRID 1873964作成日:2026年10月25日

Water → tert-Butyl 6-(benzyloxy)-3-difluoromethoxyindazole-1-carboxylate

https://huagongshe.com/reaction/1873964

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Potassium CarbonateHCID 11430—
反応物1895-39-2HCID 45051942—
反応物Tert-butyl 6-(benzyloxy)-3-oxo-2,3-dihydroindazole-1-carboxylateHCID 59370717—
溶媒DimethylformamideHCID 6228—
溶媒Ethyl AcetateHCID 8857—
生成物tert-Butyl 6-(benzyloxy)-3-difluoromethoxyindazole-1-carboxylateHCID 4528013567.5%

反応条件

温度80 °C

反応手順

Tert-butyl 6-(benzyloxy)-3-oxo-2,3-dihydroindazole-1-carboxylate (342 mg) which can be prepared according to the method described in Reference example 32, etc. and potassium carbonate (2.0887 g; manufactured by Sigma-Aldrich Co.) were suspended in dehydrated DMF (10 mL; manufactured by Kanto Chemical Co., Inc.), added with sodium chlorodifluoroacetic acid (853 mg; manufactured by Tokyo Chemical Industry, Co., Ltd.), and stirred at 80° C. for 12 hours. The reaction solution was added to water and extraction was carried out twice with ethyl acetate. The organic layer was washed twice with water and once with brine and dried over sodium sulfate. After the solvent was evaporated under reduced pressure, the residue was purified by column chromatography (“COLUMN-A”; n-hexane:ethyl acetate=100:0→87:13) to obtain the title compound (264.7 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08304443B2
出典データセットuspto-grants-2012_11
ORD IDord-4cfb48990f0746ec86dce3827fff5c7c
出典メモuspto-grants-2012_11