1,4-Diaminocyclohexane → 1-(4-(4-(4-(4-aminocyclohexylamino)-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	1,4-Diaminocyclohexane	HCID 18374	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	1-(4-(4-(4-(methylsulfinyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone	HCID 69023141	—
溶媒	Dimethyl Sulfoxide	HCID 679	—
生成物	1-(4-(4-(4-(4-aminocyclohexylamino)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone	HCID 57990390	13.1%

反応条件

温度	116 °C

反応手順

To a solution of 1-(4-(4-(4-(methylsulfinyl)-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)phenyl)piperazin-1-yl)ethanone (34 mg, 0.085 mmol) in DMSO (1 mL), 1,4-diaminocyclohexane (cis and trans mixture, 35 mg, 0.31 mmol) and diisopropylethylamine (0.060 mL, 0.35 mmol) were added. The mixture was heated at 116° C. overnight. It was then purified by HPLC to give the titled compound (5 mg). MS 449.3 (M+H); UV 208.5, 265.1, 305.5 nm.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09139581B2
出典データセット	uspto-grants-2015_09
ORD ID	ord-fc7f0ffe633449d2ba4c3cd070666f80
出典メモ	uspto-grants-2015_09