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HRID 871861作成日:2026年10月27日

Triethylamine → tert-Butyl [3-(2-chloro-5-fluorocarbonylpyrimidin-4-ylamino)propyl]-carbamate

https://huagongshe.com/reaction/871861

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Cyanuric fluorideHCID 12664—
反応物4-(3-tert-Butoxycarbonylaminopropylamino)-2-chloropyrimidine-5-carboxylic acidHCID 86673137—
溶媒DichloromethaneHCID 6344—
生成物tert-Butyl [3-(2-chloro-5-fluorocarbonylpyrimidin-4-ylamino)propyl]-carbamateHCID 8667313998%

反応手順

To a suspension of 4.91 g (14.85 mmol) of the product prepared in step 11.1 in 75 mL of dichloromethane are added 2.07 g (14.85 mmol) of triethylamine and then 1.88 mL (22.28 mmol) of cyanuric fluoride. The mixture is stirred at room temperature for 2 hours and the solution is diluted with 100 mL of dichloromethane. The organic phase is washed three times with 100 mL of ice-cold aqueous NaHCO3, dried over MgSO4, filtered and concentrated under vacuum. 4.56 g of the expected product are obtained, and are used directly in the following step. Yield=98%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08975250B2
出典データセットuspto-grants-2015_03
ORD IDord-15ab6af9169a447cab03022dd481ae2a
出典メモuspto-grants-2015_03