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HRID 490905作成日:2026年10月25日

1,2-Dichloroethane → 2,2-Dimethylpropanoyl-ethyl-6-methyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridine-5-carbohydrazide

https://huagongshe.com/reaction/490905

反応式

関与物質

役割名称HCID仕込み量
反応物1,2-DichloroethaneHCID 11—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物2,2-DimethylpropanehydrazideHCID 545147—
反応物1-Ethyl-6-methyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acidHCID 57675187—
溶媒DimethylformamideHCID 6228—
生成物2,2-Dimethylpropanoyl-ethyl-6-methyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridine-5-carbohydrazideHCID 8660898079.9%

反応手順

Intermediate 60 (0.255 g, 0.84 mmol), EDC (0.225 g, 1.17 mmol) and HOBT (0.136 g, 1.0 mmol) in DMF (5 ml) was stirred at 20° C. for 75 minutes. Pivalic acid hydrazide (0.107 g, 0.92 mmol) was added and stirring continued for 18 hours. The reaction mixture was concentrated in vacuo and the residue partitioned between DCM and water. The organic phase was washed with aqueous sodium hydrogen carbonate then evaporated in vacuo to afford Intermediate 61 as a white solid (0.27 g).). LCMS showed MH+=403; TRET=2.13 min.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07528148B2
出典データセットuspto-grants-2009_05
ORD IDord-ca21e630afde4d4291aae7deb4001f10
出典メモuspto-grants-2009_05