Ethanolamine → [4-Amino-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-5-thiazolyl][4-(2-hydroxyethyl)amino-3-nitrophenyl]methanone

関与物質

役割	名称	HCID	仕込み量
反応物	Ethanolamine	HCID 700	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	[4-Amino-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-5-thiazolyl](4-chloro-3-nitrophenyl)methanone	HCID 10162409	—
溶媒	1-Butanol	HCID 263	—
生成物	[4-Amino-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-5-thiazolyl][4-(2-hydroxyethyl)amino-3-nitrophenyl]methanone	HCID 21958939	28%

反応条件

温度	100 °C

反応手順

A mixture of [4-amino-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-5-thiazolyl](4-chloro-3-nitrophenyl)methanone (of Example 15; 0.25 g, 0.53 mmol), ethanolamine (0.13 mL, 2.12 mmol), N,N-diisopropylethylamine (Aldrich) (0.37 mL, 2.12 mmol) in n-butanol (10 mL) was heated at 100° C. overnight. The solvent was evaporated in vacuo and the residue was chromatographed on silica gel using MeOH/CH2Cl2 (1/9) as the eluent to afford 73 mg (28% yield) of the title compound. Mass spectrum (ES) MH+=498.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07094896B2
出典データセット	uspto-grants-2006_08
ORD ID	ord-514f448472b6432cb9ba9c7ab9748ad1
出典メモ	uspto-grants-2006_08