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HRID 427301作成日:2026年10月26日

5-Amino-1-methyl-1H-pyrazole-4-carbonitrile → 4-Methoxy-2-trifluoromethylbenzothiazole-7-carboxylic acid (4-cyano-2-methyl-2H-pyrazol-3-yl)amide

https://huagongshe.com/reaction/427301

反応式

関与物質

役割名称HCID仕込み量
反応物5-Amino-1-methyl-1H-pyrazole-4-carbonitrileHCID 219740—
反応物Sodium bis(trimethylsilyl)amideHCID 2724254—
反応物Methoxy-2-trifluoromethylbenzothiazole-7-carboxylic acid 4-nitrophenyl esterHCID 69689660—
溶媒DimethylformamideHCID 6228—
溶媒TetrahydrofuranHCID 8028—
生成物4-Methoxy-2-trifluoromethylbenzothiazole-7-carboxylic acid (4-cyano-2-methyl-2H-pyrazol-3-yl)amideHCID 1013442234.8%

反応手順

A solution of 5-amino-1-methyl-1H-pyrazole-4-carbonitrile (93 mg) in dimethyl formamide (10 ml) was treated with a solution of sodium hexamethyldisilazide in tetrahydrofuran (0.76 ml, 1.0M). After three minutes the mixture was treated with 4-methoxy-2-trifluoromethylbenzothiazole-7-carboxylic acid 4-nitrophenyl ester (150 mg) and the reaction stirred at room temperature for 2 hours. The solvent was removed in vacuo. Purification by flash chromatography (eluent ethyl acetate) to yield the title compound as an off-white solid (50 mg). TLC Rf 0.48 (ethyl acetate); MS found M+1 382.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06313116B1
出典データセットuspto-grants-2001_11
ORD IDord-e5d06c294e4242d0a0167a947c4a05cb
出典メモuspto-grants-2001_11