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HRID 2353968作成日:2026年10月27日

Pyridine → 5-[Acetyl-(3,5-bis-trifluoromethyl-benzyl)-amino]-8-chloro-2,3,4,5-tetrahydro-benzo[b]azepine-1-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/2353968

反応式

関与物質

役割名称HCID仕込み量
反応物PyridineHCID 1049—
反応物Acetyl chlorideHCID 6367—
反応物5-(3,5-Bis-trifluoromethyl-benzylamino)-8-chloro-2,3,4,5-tetrahydro-benzo[b]azepine-1-carboxylic acid tert-butyl esterHCID 86616082—
溶媒DichloromethaneHCID 6344—
生成物5-[Acetyl-(3,5-bis-trifluoromethyl-benzyl)-amino]-8-chloro-2,3,4,5-tetrahydro-benzo[b]azepine-1-carboxylic acid tert-butyl esterHCID 5900310771%

反応手順

Add acetyl chloride (0.3 mmol) followed by pyridine (0.3 mmol) to a solution of 5-(3,5-Bis-trifluoromethyl-benzylamino)-8-chloro-2,3,4,5-tetrahydro-benzo[b]azepine-1-carboxylic acid tert-butyl ester (0.05 g, 0.1 mmol) in dichloromethane (1 mL). After stirring at room temperature for 24 h remove solvent under vacuum. Chromatograph the product over silica gel using ethyl acetate/hexane (10-40%) to elute. This affords the title compound (0.04 g, 71%) as an oil which foams under vacuum: MS (ES+): 563 (M−H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07749992B2
出典データセットuspto-grants-2010_07
ORD IDord-5b297eeb3da74fba8a7fb3a7e63c2da1
出典メモuspto-grants-2010_07