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HRID 20564作成日:2026年10月23日

Triethylamine → 3-hydroxy-5-[(1S)-2-hydroxy-1-methylethoxy]-N-(5-methyl-1,3-thiazol-2-yl)benzamide

https://huagongshe.com/ja/reaction/20564

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物TriethylsilaneHCID 12052—
反応物3-(benzyloxy)-5-((1S)-2-{[tert-butyl(dimethyl)silyl]oxy}-1-methylethoxy)-N-(5-methyl-1,3-thiazol-2-yl)benzamideHCID 59346933—
触媒palladium(II) acetateHCID 167845—
溶媒DichloromethaneHCID 6344—
生成物3-hydroxy-5-[(1S)-2-hydroxy-1-methylethoxy]-N-(5-methyl-1,3-thiazol-2-yl)benzamideHCID 5934693021.4%

反応手順

Triethylamine (0.11 mL, 0.79 mmol) and triethylsilane (4.88 mL, 27.3 mmol) were added to palladium (11) acetate (56 mg, 9 mol %) in DCM (14 mL) under an atmosphere of argon. The reaction was stirred for 15 mins then 3-(benzyloxy)-5-((1S)-2-{[tert-butyl(dimethyl)silyl]oxy}-1-methylethoxy)-N-(5-methyl-1,3-thiazol-2-yl)benzamide (1.4 g, 2.73 mmol) in DCM (14 mL) added dropwise and stirred for a further 48 hours. The reaction was filtered through celite and the filtrate concentrated in vacuo to give a residue which was chromatographed on silica, eluting with a gradient of 50-100% ethyl acetate in isohexane, to give the desired compound (0.18 g).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07745475B2
出典データセットuspto-grants-2010_06
ORD IDord-a834994161f4422b977882c441c78710
出典メモuspto-grants-2010_06