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HRID 517373作成日:2026年10月26日

Water → Travoprost

https://huagongshe.com/reaction/517373

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物Isopropyl iodideHCID 6362—
反応物Potassium CarbonateHCID 11430—
反応物FluprostenolHCID 5311100—
溶媒DimethylformamideHCID 6228—
溶媒Ethyl AcetateHCID 8857—
生成物TravoprostHCID 528222683.3%

反応条件

温度80 °C

反応手順

A solution of crude Travoprost acid (1.1 g from Example 9) in DMF (11 mL) was treated with K2CO3 (0.90 g, 6.5 mmol) and 2-iodopropane (0.74 g, 4.4 mmol). This mixture was then stirred at 80° C. for 2 hr under an atmosphere of nitrogen (TLC monitoring). Water (30 mL) and ethyl acetate (30 mL) were added and the mixture was stirred for 10 min. The aqueous layer was separated and extracted with ethyl acetate (30 mL), and the combined organic layer was dried over magnesium sulfate and concentrated under reduced pressure to give 1.0 g of crude Travoprost. The crude Travoprost was purified by column chromatography and then concentrated under reduced pressure to provide 0.89 g of Travoprost (78.3% yield, 2 steps). UPLC (ACQUITY UPLC HSS C18) analysis of the product showed that no isomer and impurities were detectable.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09115109B2
出典データセットuspto-grants-2015_08
ORD IDord-b01c344131ba4eb3ab2d88be4fe851b3
出典メモuspto-grants-2015_08