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HRID 76193作成日:2026年10月25日

4-Iodo-2-(methylthio)pyrimidine → N-{1-Methyl-2-[4-(2-methylsulfanyl-pyrimidin-4-ylethynyl)-phenyl]-ethyl}acetamide

https://huagongshe.com/reaction/76193

反応式

関与物質

役割名称HCID仕込み量
反応物4-Iodo-2-(methylthio)pyrimidineHCID 3858901—
反応物N-(1-(4-ethynylphenyl)propan-2-yl)acetamideHCID 86669621—
触媒HCID 178418476HCID 178418476—
溶媒WaterHCID 962—
溶媒Sec-ButylamineHCID 24874—
生成物N-{1-Methyl-2-[4-(2-methylsulfanyl-pyrimidin-4-ylethynyl)-phenyl]-ethyl}acetamideHCID 66611369—

反応手順

To 0.52 g (2.58 mmol) N-[2-(4-ethynyl-phenyl)-1-methyl-ethyl]-acetamide (I58.3) and 0.50 g (1.98 mmol) 4-iodo-2-(methylthio)pyrimidine in 3 mL sec-butylamine and 3 mL water are added 0.14 g (0.20 mmol) bis(triphenylphosphine)dichloro-palladium and the mixture is stirred at r.t. over night. The reaction mixture is diluted with water and extracted with DCM. The organic layer is dried with Na2SO4 and the solvent is removed in vacuo. The residue is purified by column chromatography (silica gel, DCM/MeOH 96/4). The resulting product is triturated with diethylether.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08835472B2
出典データセットuspto-grants-2014_09
ORD IDord-81d7551219d24e2784d8aa15c266cd1c
出典メモuspto-grants-2014_09