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HRID 394411作成日:2026年10月25日

Cesium carbonate → [Rac]-2-ethoxy-3-{4-[2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethoxy]-5,6,7,8-tetrahydro-naphthalen-1-yl}-propionic acid methyl ester

https://huagongshe.com/reaction/394411

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium carbonateHCID 10796—
反応物Thiazole, 5-(chloromethyl)-2-[4-(trifluoromethyl)phenyl]-HCID 22647608—
反応物[Rac]-2-ethoxy-3-(4-hydroxy-5,6,7,8-tetrahydro-naphthalen-1-yl)-propionic acid methyl esterHCID 68617427—
溶媒DimethylformamideHCID 6228—
生成物[Rac]-2-ethoxy-3-{4-[2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethoxy]-5,6,7,8-tetrahydro-naphthalen-1-yl}-propionic acid methyl esterHCID 68617211—

反応手順

In analogy to the procedure described in 14 b], [rac]-2-ethoxy-3-(4-hydroxy-5,6,7,8-tetrahydro-naphthalen-1-yl)-propionic acid methyl ester (example 2 c]) was reacted with 5-chloromethyl-2-(4-trifluoromethyl-phenyl)-thiazole (prepared from [2-(4-trifluoromethyl-phenyl)-thiazol-5-yl]-methanol [PCT Int. Appl. (2002), WO 02/62774 A1] and methanesulfonyl chloride, triethylamine in dichloromethane) in N,N-dimethylformamide in the presence of cesium carbonate to give [rac]-2-ethoxy-3-{4-[2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethoxy]-5,6,7,8-tetrahydro-naphthalen-1-yl}-propionic acid methyl ester, which was further saponified in analogy to the procedure described in example 1 e], to yield [rac]-2-ethoxy-3-{4-[2-(4-trifluoromethyl-phenyl)-thiazol-5-ylmethoxy]-5,6,7,8-tetrahydro-naphthalen-1-yl}-propionic acid as light yellow solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US06809110B2
出典データセットuspto-grants-2004_10
ORD IDord-aa4cc4cdf31b4d99a6dd3edf245970e2
出典メモuspto-grants-2004_10