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HRID 890304作成日:2026年10月27日

1,1,3,3-Tetraethoxypropane → (2Rs,5rs)-2-{3-[5-(4-fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-propyl}-pyrimidine

https://huagongshe.com/reaction/890304

反応式

関与物質

役割名称HCID仕込み量
反応物1,1,3,3-TetraethoxypropaneHCID 67147—
反応物(2Rs,5rs)-4-[5-(4-fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-n-butyramidineHCID 22250424—
溶媒DimethylformamideHCID 6228—
生成物(2Rs,5rs)-2-{3-[5-(4-fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-propyl}-pyrimidineHCID 2225043420%

反応手順

A stirred solution of (2RS,5RS)-4-[5-(4-fluoro-phenyl)-1-(toluene-4-sulfonyl)-pyrrolidin-2-yl]-N-butyramidine (0.33 g, 0.82 mmol) in 1,1,3,3-tetraethoxy-propane (7 ml) and DMF (1.5 ml) was heated for 1 h at 150° C. Evaporation and purification by column chromatography on silica gel (dichloromethane/MeOH 98:2) yielded the title compound (73 mg, 20%) as a light brown oil, MS: m/e=440.2 (M+H+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06995182B2
出典データセットuspto-grants-2006_02
ORD IDord-a0e058f0bd3e4f9e90ee8afd578557ff
出典メモuspto-grants-2006_02