Water → 2-[(2-amino-5-{[(1S)-1-phenylethyl]thio}[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentan-1-ol

関与物質

役割	名称	HCID	仕込み量
反応物	Water	HCID 962	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	D(-)-Leucinol	HCID 2724002	—
反応物	(S)-7-chloro-5-((1-phenylethyl)thio)thiazolo[4,5-d]pyrimidin-2-amine	HCID 86622916	—
溶媒	N-methyl-2-pyrrolidone	HCID 13387	—
生成物	2-[(2-amino-5-{[(1S)-1-phenylethyl]thio}[1,3]thiazolo[4,5-d]pyrimidin-7-yl)amino]-4-methylpentan-1-ol	HCID 86622917	55.1%

反応条件

温度	120 °C

反応手順

DIPEA (400 mg, 3 mmol) and D-leucinol (400 mg, 3.4 mmol) were added to 7-chloro-5-{[(1S)-1-phenylethyl]thio}[1,3]thiazolo[4,5-d]pyrimidin-2-amine (300 mg, 0.9 mmol) in NMP (6 mL) and the mixture was heated to 120° C. for 24 h. The mixture was poured into water and extracted with ethyl acetate. The organic phase was dried (MgSO4), evaporated and the residue was purified by flash column chromatography (EtOAc) to give the title compound (200 mg, 54% yield).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US09440992B2
出典データセット	uspto-grants-2016_09
ORD ID	ord-6e89b2ba57dc4b95875c7e426c7ec9a5
出典メモ	uspto-grants-2016_09