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HRID 914356作成日:2026年10月27日

Water → 2-[(4-{2-[(6-Chloropyridazin-3-yl)amino]ethyl}-1,3-thiazol-2-yl)thio]-2-methylpropionic acid tert-butyl ester

https://huagongshe.com/reaction/914356

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物3,6-DichloropyridazineHCID 67331—
反応物DiisopropylethylamineHCID 81531—
反応物2-{[4-(2-Aminoethyl)-1,3-thiazol-2-yl]thio}-2-methylpropionic acid tert-butyl esterHCID 59759449—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物2-[(4-{2-[(6-Chloropyridazin-3-yl)amino]ethyl}-1,3-thiazol-2-yl)thio]-2-methylpropionic acid tert-butyl esterHCID 5975921080.2%

反応条件

温度130 °C

反応手順

2-{[4-(2-Aminoethyl)-1,3-thiazol-2-yl]thio}-2-methylpropionic acid tert-butyl ester (5.0 g) synthesized in Example 7 and 3,6-dichloropyridazine (4.92 g) were dissolved in N-methylpyrrolidone (25 mL), diisopropylethylamine (4.27 g) was added, and the mixture was heated at 130° C. with stirring for 8 hr. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure, and the residue was purified by silica gel chromatography (elution solvent; hexane:ethyl acetate=2:1 to 1:1) to give the title compound (5.5 g) as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08026370B2
出典データセットuspto-grants-2011_09
ORD IDord-cbc7d7548e734800954ecd370ab51faa
出典メモuspto-grants-2011_09