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HRID 72511作成日:2026年10月25日

Triethylamine → Methyl 4-(1-(5-chloro-2-(3-((4-fluoro-2-methylphenyl)amino)azetidin-1-yl)nicotinamido)cyclopropyl)benzoate

https://huagongshe.com/reaction/72511

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物N-(4-fluoro-2-methylphenyl)azetidin-3-amineHCID 65958632—
反応物Methyl 4-(1-(2,5-dichloronicotinamido)cyclopropyl)benzoateHCID 86697873—
溶媒MeOH tetrahydrofuranHCID 21899815—
生成物Methyl 4-(1-(5-chloro-2-(3-((4-fluoro-2-methylphenyl)amino)azetidin-1-yl)nicotinamido)cyclopropyl)benzoateHCID 67958192—

反応条件

温度75 °C

反応手順

To a solution of N-(4-fluoro-2-methylphenyl)azetidin-3-amine (D55) and triethylamine (0.14 ml, 1.04 mmol) in tetrahydrofuran/methanol (3 ml/1 ml) methyl 4-(1-(2,5-dichloronicotinamido)cyclopropyl)benzoate (D97) (253 mg, 0.693 mmol) was added and the resulting mixture was heated 24 h at 75° C. The residue obtained after solvent evaporation, was purified by Biotage SNAP-Si (10 g) cartridge eluting with eluting with a mixture dichloromethane/ethylacetate from 95/5 to 80/20. Collected fractions, after solvent evaporation afforded the title compound (D168) (105 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08828987B2
出典データセットuspto-grants-2014_09
ORD IDord-087db1940e3d4e408bbd2d90170e5faf
出典メモuspto-grants-2014_09