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HRID 78219作成日:2026年10月26日

Sodium hydride → 3-(1-(6-Phenoxy-pyridin-3-ylmethyl)-1H-pyrazol-4-yl)-pyridin-2,6-diamine

https://huagongshe.com/reaction/78219

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium hydrideHCID 24758—
反応物5-Chloromethyl-2-phenoxy-pyridineHCID 13253476—
反応物3-(1H-pyrazol-4-yl)-pyridine-2,6-diamineHCID 59255172—
溶媒DimethylformamideHCID 6228—
生成物3-(1-(6-Phenoxy-pyridin-3-ylmethyl)-1H-pyrazol-4-yl)-pyridin-2,6-diamineHCID 5925532425.2%

反応手順

To an N,N-dimethylformamide (5.00 mL) solution of 3-(1H-pyrazol-4-yl)-pyridine-2,6-diamine (30.0 mg, 0.171 mmol) described in Manufacturing Example 36-1-2 was added sodium hydride (7.52 mg, 0.188 mmol, 60% in oil) on an ice bath (0° C.) under nitrogen atmosphere, which was stirred for 10 minutes at room temperature. Thereafter, 5-chloromethyl-2-phenoxy-pyridine (59.9 mg, 0.273 mmol) described in Manufacturing Example 193-1-2 was added to the above mixture, which was stirred for 30 minutes at room temperature. The reaction mixture was partitioned into ethyl acetate and water at room temperature. The organic layer was washed with water and saturated aqueous sodium chloride and dried over anhydrous magnesium sulfate, and the solvent was evaporated under a reduced pressure. The residue was purified by NH silica gel column chromatography (ethyl acetate) to obtain the title compound (15.4 mg, 25.2%).

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-b7753dcec1a24e5bacb72e27b054c634
出典メモuspto-grants-2014_09