Chlorotrimethylsilane → 1-(4-(4-(4-(1H-indazol-6-ylamino)-5-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone

関与物質

役割	名称	HCID	仕込み量
反応物	Chlorotrimethylsilane	HCID 6397	—
反応物	1-[4-(4-Aminophenyl)piperazin-1-yl]ethan-1-one	HCID 736269	—
反応物	2-Chloro-N-(1H-indazol-6-yl)-5-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine	HCID 86628037	—
溶媒	1-Butanol	HCID 263	—
生成物	1-(4-(4-(4-(1H-indazol-6-ylamino)-5-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone	HCID 68580170	17.7%

反応条件

温度	115 °C

反応手順

To a mixture of 2-Chloro-N-(1H-indazol-6-yl)-5-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine (0.18 g, 0.4 mmol) and 1-(4-(4-aminophenyl)piperazin-1-yl)ethanone (0.22 g, 1 mmol) in n-butyl alcohol (2 mL) was added trimethylsilyl chloride (TMSCl) (0.026 mL, 0.2 mmol). After heating at 115° C. for 15 h, the mixture was purified by preparative HPLC to give 1-(4-(4-(4-(1H-indazol-6-ylamino)-5-methyl-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone (0.045 g).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07705004B2
出典データセット	uspto-grants-2010_04
ORD ID	ord-6cc7cd34432a4af0a55f7f2cfa81f0cf
出典メモ	uspto-grants-2010_04