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HRID 523975作成日:2026年10月25日

Glycine → FG 4592

https://huagongshe.com/reaction/523975

反応式

関与物質

役割名称HCID仕込み量
反応物GlycineHCID 750—
反応物Sodium GlycinateHCID 4684308—
反応物Sodium MethoxideHCID 10942334—
反応物3-Isoquinolinecarboxylic acid, 4-hydroxy-1-methyl-7-phenoxy-, methyl esterHCID 71244895—
溶媒MethanolHCID 887—
生成物FG 4592HCID 1125666486.1%

反応条件

温度110 °C

反応手順

A pressure flask was charged with 3e (30.92 g), glycine (22.52 g), methanol (155 mL), sodium methoxide solution (64.81 g) and sealed (as an alternative, sodium glycinate was used in place of glycine and sodium methoxide). The reaction was heated to about 110° C. until reaction was complete. The mixture was cooled, filtered, washed with methanol, dried under vacuum, dissolved in water and washed with ethyl acetate. The ethyl acetate was removed and to the resulting aqueous layer an acetic acid (18.0 g) solution was added. The suspension was stirred at room temperature, filtered, and the solid washed with water (3×30 mL), cold acetone (5-10° C., 2×20 mL), and dried under vacuum to obtain 2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid (Yield: 86.1%, HPLC: 99.8%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09340511B2
出典データセットuspto-grants-2016_05
ORD IDord-07705635484f42dcbae9b04aa3cbbdd9
出典メモuspto-grants-2016_05