Sodium Carbonate → (1S, 2R)-2,5-Difluoro-4'-(2-hydroxy-1-methyl-4-pyridin-3-yl-butoxy)biphenyl-4-sulfonic acid amide

関与物質

役割	名称	HCID	仕込み量
反応物	Sodium Carbonate	HCID 10340	—
反応物	4-Bromo-2,5-difluorobenzenesulfonamide	HCID 2773293	—
反応物	(1S,2R)-4-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)benzeneboronic acid	HCID 54413593	—
触媒	HCID 178418397	HCID 178418397	—
溶媒	Ethanol	HCID 702	—
生成物	(1S, 2R)-2,5-Difluoro-4'-(2-hydroxy-1-methyl-4-pyridin-3-yl-butoxy)biphenyl-4-sulfonic acid amide	HCID 57221958	36.9%

反応条件

温度	80 °C

反応手順

Prepared according to the method described in Example 12) from (1S,2R)-4-(2-hydroxy-1-methyl-4-pyridin-3-ylbutoxy)benzeneboronic acid (0.2 g, Example 33), 4-bromo-2,5-difluorobenzenesulfonamide (0.19 g, Example 37a)), ethanol (3 ml), 2M aqueous sodium carbonate (0.7 ml) and tetrakis(triphenylphosphine)palladium (0) (0.03 g) with heating at 80° C. for 3 hours. After work-up, the residue was purified by normal-phase HPLC eluting with a gradient of 0-25% ethanol in dichloromethane to give the title compound as a foam (0.11 g).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US06300352B1
出典データセット	uspto-grants-2001_10
ORD ID	ord-40aa2691177f42fb8a7f311de55bd7c5
出典メモ	uspto-grants-2001_10