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HRID 409984作成日:2026年10月25日

2-Fluorobenzoyl chloride → tert-Butyl (2-(7-(2-fluoro-4-(2-fluorobenzamido)phenoxy)thieno[3,2-b]pyridin-2-yl)-1-methyl-1H-imidazol-5-yl)methyl(2-methoxyethyl)carbamate

https://huagongshe.com/reaction/409984

反応式

関与物質

役割名称HCID仕込み量
反応物2-Fluorobenzoyl chlorideHCID 9808—
反応物DiisopropylethylamineHCID 81531—
反応物tert-Butyl (2-(7-(4-amino-2-fluorophenoxy)thieno[3,2-b]pyridin-2-yl)-1-methyl-1H-imidazol-5-yl)methyl(2-methoxyethyl)carbamateHCID 57919490—
溶媒DichloromethaneHCID 6344—
生成物tert-Butyl (2-(7-(2-fluoro-4-(2-fluorobenzamido)phenoxy)thieno[3,2-b]pyridin-2-yl)-1-methyl-1H-imidazol-5-yl)methyl(2-methoxyethyl)carbamateHCID 58236607108.3%

反応手順

To a solution of aniline 46 (300 mg, 0.569 mmol) in DCM (10 mL) at 0° C. was added DIPEA (0.199 mL, 1.137 mmol) and 2-fluorobenzoyl chloride (135 mg, 0.853 mmol) and the suspension was stirred overnight at room temperature. The reaction mixture was concentrated and the residue was partitioned between EtOAc and water. The organic layer was collected, dried and concentrated. The residue was purified using Biotage (eluent EtOAc, 25 g Silicycle HR column) to provide the title compound 356 (400 mg, 0.616 mmol, quantitative yield) as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08759522B2
出典データセットuspto-grants-2014_06
ORD IDord-09019c1bbb2a436e90cf5d9527bfd250
出典メモuspto-grants-2014_06