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HRID 77819作成日:2026年10月25日

Methanol → 3-(3-(4-(6-Methyl-pyridin-2-ylmethoxy)-benzyl)-isoxazol-5-yl)-pyridin-2-ylamine

https://huagongshe.com/reaction/77819

反応式

関与物質

役割名称HCID仕込み量
反応物MethanolHCID 887—
反応物Sodium HydroxideHCID 14798—
反応物2-(Chloromethyl)-6-methylpyridineHCID 76546—
反応物4-(5-(2-Amino-pyridin-3-yl)isoxazol-3-ylmethyl)phenolHCID 25114386—
溶媒DimethylformamideHCID 6228—
生成物3-(3-(4-(6-Methyl-pyridin-2-ylmethoxy)-benzyl)-isoxazol-5-yl)-pyridin-2-ylamineHCID 5925524751.7%

反応条件

温度60 °C

反応手順

Methanol (3 mL) and 1 N aqueous sodium hydroxide solution (0.18 mL) were added to 4-(5-(2-amino-pyridin-3-yl)isoxazol-3-ylmethyl)-phenol (50 mg, 0.19 mmol) described in Manufacturing Example 5-1-1, which was then dissolved by irradiating ultrasonic wave. This solution was concentrated under a reduced pressure. To the resulting residue were added 2-chloromethyl-6-methyl-pyridine (31.8 mg, 0.22 mmol) described in Manufacturing Example 10-1-1 and N,N-dimethylformamide (2 mL), which was stirred for 20 minutes at 60° C. The reaction solution was partitioned into water and ethyl acetate. The organic layer was separated, and the solvent was evaporated under a reduced pressure. The residue was purified by NH silica gel column chromatography (heptane:ethyl acetate=1:1) to obtain the title compound (36 mg, 51.7%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08841327B2
出典データセットuspto-grants-2014_09
ORD IDord-704b2539ac8c438197dcecae42be4879
出典メモuspto-grants-2014_09