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HRID 1012960作成日:2026年10月26日

Triethylamine → {1-[4-(4-Fluoro-phenyl)phthalazin-1-yl]piperidin-4-yl}-methyl-carbamic acid tert-butyl ester

https://huagongshe.com/reaction/1012960

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-4-(4-fluorophenyl)phthalazineHCID 2115239—
反応物4-N-Boc-4-N-Methyl-aminopiperidineHCID 2756806—
溶媒DimethylformamideHCID 6228—
溶媒DichloromethaneHCID 6344—
生成物{1-[4-(4-Fluoro-phenyl)phthalazin-1-yl]piperidin-4-yl}-methyl-carbamic acid tert-butyl esterHCID 5815712888%

反応条件

温度130 °C

反応手順

Add 1-chloro-4-(4-fluorophenyl)-phthalazine (3.00 g, 11.6 mmol) to a solution of methyl-piperidin-4-yl-carbamic acid tert-butyl ester (2.98 g, 13.9 mmol) and triethylamine (3.52 g., 34.8 mmol) in DMF (30 mL). Heat at 130° C. for 3 days. Dissolve the reaction mixture in dichloromethane and wash with brine. Dry the organic phase with sodium sulfate, filter, and concentrate under reduced pressure. Purify the resulting residue by flash chromatography (20:5:1, hexane:ethyl acetate: 2 M ammonia in methanol) to yield the title compound as a solid (4.45 g, 88%). ES/MS m/z 437.2 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07981892B2
出典データセットuspto-grants-2011_07
ORD IDord-5c9f3cc8906441889ca44d7048524c4d
出典メモuspto-grants-2011_07