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HRID 844083作成日:2026年10月25日

Triethylamine → 2-(4-Fluoro-phenoxy)-N-[4-(1-hydroxy-1-methyl-ethyl)-cyclohex-1-enylmethyl]-nicotinamide

https://huagongshe.com/reaction/844083

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物1-Chloro-2-(diethylamine)ethane hydrochlorideHCID 13363—
反応物2-(4-Fluorophenoxy)nicotinic acidHCID 605123—
反応物1-Hydroxybenzotriazole hydrateHCID 2796029—
反応物2-(4-Aminomethyl-cyclohex-3-enyl)-propan-2-olHCID 22612225—
溶媒DichloromethaneHCID 6344—
生成物2-(4-Fluoro-phenoxy)-N-[4-(1-hydroxy-1-methyl-ethyl)-cyclohex-1-enylmethyl]-nicotinamideHCID 226122069.8%

反応手順

A solution of 2-(4-Aminomethyl-cyclohex-3-enyl)-propan-2-ol (0.360 grams, 2.127 mmole), 2-diethylaminoethyl chloride hydrochloride (0.530 grams, 2.765 mmole), 2-(4-Fluoro-phenoxy)-nicotinic acid (0.645 grams, 2.765 mmole), 1-hydroxybenzotriazole hydrate (0.374 grams, 2.765 mmole) and triethyl amine (0.430 grams, 4.254 mmole) in methylene chloride (40 ml) was added and stirred over night. The mixture was concentrated and partitioned between ethyl acetate and 1 N HCl. The organic extracts were washed with saturated sodium hydrogencarbonate and brine, dried over MgSO4, filtered and concentrated to give an oil which was purified by chromatography on silica eluting with 50% ethyl acetate/hexane to 100% ethyl acetate to give a yellow oil (0.080 g); M.W. 384.455; MS 385 (M++1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06380218B1
出典データセットuspto-grants-2002_04
ORD IDord-fb963c79262b485eb439c77b6ad35565
出典メモuspto-grants-2002_04