Potassium Carbonate → Methyl 2-((S)-6-((R)-4-(2,6-dimethyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)phenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate

https://huagongshe.com/ja/reaction/237692

関与物質

役割	名称	HCID	仕込み量
反応物	Potassium Carbonate	HCID 11430	—
反応物	4-(Bromomethyl)oxane	HCID 2773286	—
反応物	Methyl 2-((S)-6-((R)-7-fluoro-4-(4-hydroxy-2,6-dimethylphenyl)-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate	HCID 86697113	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	Methyl 2-((S)-6-((R)-4-(2,6-dimethyl-4-((tetrahydro-2H-pyran-4-yl)methoxy)phenyl)-7-fluoro-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate	HCID 86697366	—

反応条件

温度	60 °C

反応手順

Methyl 2-((S)-6-((R)-7-fluoro-4-(4-hydroxy-2,6-dimethylphenyl)-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate (Intermediate 28-29) (138 mg) and 4-(bromomethyl)tetrahydro-2H-pyran (160.3 mg) were suspended in dimethylformamide (5 mL) and potassium carbonate (185.7 mg) was added. The reaction mixture was shaken for 48 h at 60° C. and than directly chromatographed by HPLC on reversed phase. The product fractions are collected and lyophilized to give the title compound. Yield: 117 mg; LC (method 23): tR=2.26 min; Mass spectrum (ESI+): m/z=561 [M+H]+.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08642585B2
出典データセット	uspto-grants-2014_02
ORD ID	ord-c9b144539c7f4adcb4d8c97575328fd6
出典メモ	uspto-grants-2014_02