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HRID 78218作成日:2026年10月25日

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

https://huagongshe.com/reaction/78218

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2-(Benzyloxy)-5-(chloromethyl)pyridineHCID 22009600—
反応物3-(1H-pyrazol-4-yl)-pyridine-2,6-diamineHCID 59255172—
溶媒DimethylformamideHCID 6228—
生成物3-(1-(6-Benzyloxy-pyridin-3-ylmethyl)-1H-pyrazol-4-yl)-pyridin-2,6-diamineHCID 5925525143%

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.), which was stirred for 30 minutes at room temperature. Thereafter, 2-benzyloxy-5-chloromethyl-pyridine (59.9 mg, 0.257 mmol) described in Manufacturing Example 191-1-2 was added to the mixture, which was stirred for 30 minutes at room temperature. The reaction mixture was partitioned into ethyl acetate and water. The organic layer was washed with water and a saturated sodium chloride aqueous solution, and dried with 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 (27.4 mg, 43.0%).

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-ff1937ed8fdc48aaa85bdf91217a1de4
出典メモuspto-grants-2014_09