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HRID 221372作成日:2026年10月26日

tert-Butyl 4-sulfanylpiperidine-1-carboxylate → 4-(3-Pyridin-4-yl-[1,2,4]oxadiazol-5-ylmethylsulfanyl)piperidine-1-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/221372

反応式

関与物質

役割名称HCID仕込み量
反応物tert-Butyl 4-sulfanylpiperidine-1-carboxylateHCID 21906090—
反応物Potassium tert-butoxideHCID 23665647—
反応物Methanesulfonic acid 3-pyridin-4-yl-[1,2,4]oxadiazol-5-ylmethyl esterHCID 57954388—
溶媒Diethyl EtherHCID 3283—
溶媒TetrahydrofuranHCID 8028—
生成物4-(3-Pyridin-4-yl-[1,2,4]oxadiazol-5-ylmethylsulfanyl)piperidine-1-carboxylic acid tert-butyl esterHCID 57954409—

反応手順

t-BuOK (92 mg, 823 μmol) and methanesulfonic acid 3-pyridin-4-yl-[1,2,4]oxadiazol-5-ylmethyl ester (Preparation 12, 150 mg, 588 μmol) were added to a stirred solution of 4-mercaptopiperidine-1-carboxylic acid tert-butyl ester (191 mg, 881 mol) in anhydrous THF (10 ml). After 100 min, the reaction mixture was diluted with Et2O, before being washed with NaHCO3 and brine. The organic layer was dried (MgSO4), filtered, and concentrated, then the residue was purified by column chromatography (IH-EtOAc, 3:2) to afford the title compound: RT=3.77 min; m/z (ES+)=377.2 [M+H]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08207147B2
出典データセットuspto-grants-2012_06
ORD IDord-bad805c3d4a949ff81a3f21fa38fd134
出典メモuspto-grants-2012_06