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HRID 278649作成日:2026年10月27日

Dichloromethane → [4-(5-(Cyclopropyl-amino)-8,8-dimethyl-5,6,7,8-tetrahydro-naphthalene-2-yl-ethynyl)-2-fluoro-phenyl] acetic acid ethyl ester

https://huagongshe.com/reaction/278649

反応式

関与物質

役割名称HCID仕込み量
反応物DichloromethaneHCID 6344—
反応物CyclopropylamineHCID 69828—
反応物Sodium cyanoborohydrideHCID 5003444—
反応物[2-Fluoro-4-(8,8-dimethyl-5-oxo-5,6,7,8-tetrahydronaphthalene-2-ylethynyl)phenyl]acetic acid ethyl esterHCID 69548870—
溶媒Acetic AcidHCID 176—
溶媒AcetonitrileHCID 6342—
溶媒HexaneHCID 8058—
溶媒Ethyl AcetateHCID 8857—
生成物[4-(5-(Cyclopropyl-amino)-8,8-dimethyl-5,6,7,8-tetrahydro-naphthalene-2-yl-ethynyl)-2-fluoro-phenyl] acetic acid ethyl esterHCID 69548141—

反応手順

Following general procedure G and using [2-fluoro-4-(8,8-dimethyl-5-oxo-5,6,7,8-tetrahydro-naphthalene-2-ylethynyl) phenyl]acetic acid ethyl ester (Compound 14, 0.258 g, 0.68 mmol), dichloromethane (4 mL), acetonitrile(2 mL), cyclopropyl amine(1 mL, 14.45 mmol), acetic acid (1 mL)and sodium cyanoborohydride (0.266 g, 4.23 mmol) followed by flash column chromatography over silica gel (230-400 mesh) using 16-20-25% ethyl acetate in hexane as the eluent, the title compound was obtained as a pale yellow oil (0.21 g, 73%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06359135B1
出典データセットuspto-grants-2002_03
ORD IDord-4520212d4505447d9193d13a60c3b107
出典メモuspto-grants-2002_03