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HRID 11700作成日:2026年10月25日

Glycine, N-methyl-, methyl ester, hydrochloride (1:1) → [(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-benzyl)-methyl-amino]-acetic Acid Methyl Ester

https://huagongshe.com/reaction/11700

反応式

関与物質

役割名称HCID仕込み量
反応物Glycine, N-methyl-, methyl ester, hydrochloride (1:1)HCID 83544—
反応物Sodium triacetoxyborohydrideHCID 5049666—
反応物(2R,5S)-5-Chloro-2-{2-[4-(4-fluoro-benzyl)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-benzaldehydeHCID 53673807—
溶媒MethanolHCID 887—
生成物[(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-benzyl)-methyl-amino]-acetic Acid Methyl EsterHCID 69655231—

反応手順

To a solution of 5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-benzaldehyde (0.10 g, 0.24 mmol) in methanol (2.5 ml) was added sarcosine methyl ester hydrochloride salt (0.10 g, 0.72 mmol) followed by sodium triacetoxyborohydride (0.155 g, 0.73 mmol). After 15 hours the solvent was removed and the resultant solid taken up in methylene chloride. After washing with pH 7 phosphate buffer (0.05 M) and saturated aqueous sodium chloride the organic layer was dried over magnesium sulfate. After filtration and concentration the title compound was isolated by chromatography on silica gel (0.051 g).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07098212B2
出典データセットuspto-grants-2006_08
ORD IDord-bc9c26b9cc494c06af51d41a336564d4
出典メモuspto-grants-2006_08