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HRID 72501作成日:2026年10月25日

Trifluoroacetic acid methylene chloride → Methyl 4-(1-(5-chloro-2-(3-(3-(piperazin-1-yl)phenoxy)azetidin-1-yl)nicotinamido)cyclopropyl)benzoate

https://huagongshe.com/reaction/72501

反応式

関与物質

役割名称HCID仕込み量
反応物Trifluoroacetic acid methylene chlorideHCID 21863450—
反応物Tert-butyl 4-(3-((1-(5-chloro-3-((1-(4-(methoxycarbonyl)phenyl)cyclopropyl)carbamoyl)pyridin-2-yl)azetidin-3-yl)oxy)phenyl)piperazine-1-carboxylateHCID 67958770—
溶媒DichloromethaneHCID 6344—
生成物Methyl 4-(1-(5-chloro-2-(3-(3-(piperazin-1-yl)phenoxy)azetidin-1-yl)nicotinamido)cyclopropyl)benzoateHCID 6795860595.3%

反応手順

To a cooled solution of tert-butyl 4-(3-((1-(5-chloro-3-((1-(4-(methoxycarbonyl)phenyl)cyclopropyl)carbamoyl)pyridin-2-yl)azetidin-3-yl)oxy)phenyl)piperazine-1-carboxylate (130 mg, 0.196 mmol) in dichloromethane (1 ml) a mixture trifluoroacetic acid/dichloromethane (3 ml/1 ml) was added and the resulting mixture stirred for 15 min. Solvents were evaporated in vacuo to afford a residue that was loaded on SPE-SCX (5 g) cartridge. Ammonia fractions after solvent evaporation afforded the title compound (D156) (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-5f00722bb44845288b29d3403d13c1dc
出典メモuspto-grants-2014_09