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HRID 1404277作成日:2026年10月25日

Sodium Carbonate → (4-{4-[5-(6-Trifluoromethyl-pyridin-3-ylamino)-pyrazin-2-yl]-phenyl}-cyclohexyl)-acetic acid methyl ester

https://huagongshe.com/reaction/1404277

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物Methyl 2-[4-[4-(5-bromopyridin-2-yl)phenyl]cyclohexyl]acetateHCID 66615782—
反応物(5-Bromopyrazin-2-yl)-(6-trifluoromethyl-pyridin-3-yl)-amineHCID 86634697—
触媒HCID 178418397HCID 178418397—
溶媒1,2-DimethoxyethaneHCID 8071—
生成物(4-{4-[5-(6-Trifluoromethyl-pyridin-3-ylamino)-pyrazin-2-yl]-phenyl}-cyclohexyl)-acetic acid methyl esterHCID 66615921—

反応条件

温度130 °C

反応手順

A solution of (5-Bromo-pyrazin-2-yl)-(6-trifluoromethyl-pyridin-3-yl)-amine (0.072 g) and {4-[4-(5-bromo-pyridin-2-yl)-phenyl]-cyclohexyl}-acetic acid methyl ester (0.087 g) in 2 Ml DME was charged with 2 M sodium carbonate (1 Ml) and Pd(PPh3)4 (0.027 g, 0.1 equiv). The biphasic mixture was sparged with nitrogen for 3 min, then stirred at 130° C. under microwave heating for 30 min. The reaction was partitioned between EtOAc and water, and the organic extracts were dried over magnesium sulphate and concentrated in vacuo. Purification by silica gel chromatography (33% EtOAc in hexanes) afforded the title compound: (M+H)+ 471.2.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08912208B2
出典データセットuspto-grants-2014_12
ORD IDord-81eaacc2fe6b4f07af9cfbf12be10132
出典メモuspto-grants-2014_12