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HRID 2089674作成日:2026年10月27日

1-Propanesulfonic acid → 3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}-phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester propanesulfonate

https://huagongshe.com/reaction/2089674

反応式

関与物質

役割名称HCID仕込み量
反応物1-Propanesulfonic acidHCID 78938—
反応物3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl esterHCID 67471184—
溶媒Ethyl AcetateHCID 8857—
生成物3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}-phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester propanesulfonateHCID 86677406—

反応手順

At room temperature, 3-methoxy-2,2-dimethylpropionic acid 5-[(R)-[3-(2-acetoxyethoxy)-2-fluoro-5-methoxyphenyl]-(4-{amino[2-methylallyloxycarbonylimino]methyl}phenylamino)methyl]-2-pyrimidin-2-yl-2H-[1,2,4]triazol-3-yloxymethyl ester (Example 6f, 100 mg) was dissolved in ethyl acetate (10 mL), a solution of 1-propanesulfonic acid [CAS No. 5284-66-2] (13.5 mg) in ethyl acetate (1 mL) was added dropwise thereto. The resulting mixture was stirred at room temperature for 22 hours, and the precipitated solid was filtered. The solids recovered by filtration were washed with ethyl acetate and TBME, and dried. The captioned compound (90 mg) was obtained.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08436009B2
出典データセットuspto-grants-2013_05
ORD IDord-2e44d4a1045040d58a204d93b19e7e9b
出典メモuspto-grants-2013_05