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HRID 1410067作成日:2026年10月27日

Diisopropylethylamine → N-(3-((1R,5S)-8-oxa-3-azabicyclo[3.2.1]octan-3-yl)phenyl)-5-chlorothiazolo[5,4-d]pyrimidin-7-amine

https://huagongshe.com/reaction/1410067

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物5,7-Dichlorothiazolo(5,4-d)pyrimidineHCID 609639—
反応物3-((1R,5S)-8-oxa-3-azabicyclo[3.2.1]octan-3-yl)anilineHCID 68379258—
溶媒Dimethyl SulfoxideHCID 679—
溶媒WaterHCID 962—
生成物N-(3-((1R,5S)-8-oxa-3-azabicyclo[3.2.1]octan-3-yl)phenyl)-5-chlorothiazolo[5,4-d]pyrimidin-7-amineHCID 8667178686%

反応条件

温度30 °C

反応手順

The mixture of 3-((1R,5S)-8-oxa-3-azabicyclo[3.2.1]octan-3-yl)aniline (0.061 g, 0.3 mmol), 5,7-dichlorothiazolo[5,4-d]pyrimidine (0.061 g, 0.3 mmol) and DIPEA (0.046 g, 0.36 mmol) in DMSO (10 mL) was heated to 30° C. for 2 h. Then it was diluted with water and extracted with ethyl acetate (3×10 mL), the organics were dried and concentrated. The residue was purified by column chromatography (silica gel, 200˜300 mesh, eluting with MeOH:DCM=1:80) to afford N-(3-((1R,5S)-8-oxa-3-azabicyclo[3.2.1]octan-3-yl)phenyl)-5-chlorothiazolo[5,4-d]pyrimidin-7-amine (0.095 g, 86%) as a yellow solid. LC-MS: 374 [M+H]+, tR=1.66 min.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08921383B2
出典データセットuspto-grants-2014_12
ORD IDord-26f0d20983bd490c9364c0ed844e1b01
出典メモuspto-grants-2014_12