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HRID 238650作成日:2026年10月26日

Triphenylphosphine → [4-(5-Ethanesulfonyl-3-ethyl-pyridin-2-yloxy)-6-fluoro-3-methyl-naphthalen-2-yl]-acetic acid methyl ester

https://huagongshe.com/reaction/238650

反応式

関与物質

役割名称HCID仕込み量
反応物TriphenylphosphineHCID 11776—
反応物Potassium Phosphate, TribasicHCID 62657—
反応物Ethylboronic acidHCID 521157—
反応物[4-(3-Bromo-5-ethanesulfonyl-pyridin-2-yloxy)-6-fluoro-3-methyl-naphthalen-2-yl]-acetic acid methyl esterHCID 59326492—
触媒HCID 178418476HCID 178418476—
溶媒TolueneHCID 1140—
生成物[4-(5-Ethanesulfonyl-3-ethyl-pyridin-2-yloxy)-6-fluoro-3-methyl-naphthalen-2-yl]-acetic acid methyl esterHCID 5932658647.6%

反応条件

温度100 °C

反応手順

A mixture of [4-(3-bromo-5-ethanesulfonyl-pyridin-2-yloxy)-6-fluoro-3-methyl-naphthalen-2-yl]-acetic acid methyl ester (42 mg, 0.085 mmol), ethylboronic acid (15 mg, 0.20 mmol), bis(triphenylphosphine)dichloropalladium(II) (7.0 mg, 0.01 mmol), potassium phosphate (64 mg, 0.30 mmol), triphenylphosphine (15.2 mg, 0.05 mmol) and toluene (1 mL) was stirred at 100° C. overnight under an argon atmosphere. The resulting mixture was filtered. The filtrate was concentrated in vacuo. The residue was purified by preparative TLC (20% ethyl acetate in petroleum ether) to afford [4-(5-ethanesulfonyl-3-ethyl-pyridin-2-yloxy)-6-fluoro-3-methyl-naphthalen-2-yl]-acetic acid methyl ester (18 mg, 47.6%) as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08642629B2
出典データセットuspto-grants-2014_02
ORD IDord-cbf8dc933ca44dbaa04705673f6fb29c
出典メモuspto-grants-2014_02