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HRID 623666作成日:2026年10月25日

Morpholine → 4-{4-[3-(2,4-bis-benzyloxy-5-isopropyl-phenyl)-3H-[1,2,3]triazol-4-yl]-benzyl}-morpholine

https://huagongshe.com/reaction/623666

反応式

関与物質

役割名称HCID仕込み量
反応物MorpholineHCID 8083—
反応物Methanesulfonyl chlorideHCID 31297—
反応物{4-[3-(2,4-bis-benzyloxy-5-isopropyl-phenyl)-3H-[1,2,3]triazol-4-yl]-phenyl}-methanolHCID 67985193—
溶媒DimethylformamideHCID 6228—
溶媒DichloromethaneHCID 6344—
生成物4-{4-[3-(2,4-bis-benzyloxy-5-isopropyl-phenyl)-3H-[1,2,3]triazol-4-yl]-benzyl}-morpholineHCID 6798541780%

反応条件

温度0 °C

反応手順

TEA (160 μl, 1.17 mmol) and MsCl (90 μl, 1.17 mmol) were added to a solution of {4-[3-(2,4-bis-benzyloxy-5-isopropyl-phenyl)-3H-[1,2,3]triazol-4-yl]-phenyl}-methanol (200 mg, 0.39 mmol) in DCM (5 ml) at 0° C. The solution was stirred for 30 minutes at 0° C. and for 12 hours at RT. The solvent was removed under reduced pressure and the reaction crude was dissolved in DMF (3 ml). Morpholine (1.17 mmol) and TEA (160 μl, 1.17 mmol) were added and the reaction mixture was stirred for 12 hours at RT. After standard work-up with AcOEt (4×30 ml) and washing with H2O (2×30 mL) and brine (2×30 ml), the solvent was evaporated under reduced pressure and the crude reaction mixture was purified by column chromatography (PE/AcOEt:20/80) to obtain the desired adduct as an oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09302998B2
出典データセットuspto-grants-2016_04
ORD IDord-c8c63ff405f8485cbd1e1dae2b349f79
出典メモuspto-grants-2016_04