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HRID 237415作成日:2026年10月26日

Paclitaxel → Fmoc-Leu PABC Paclitaxel

https://huagongshe.com/reaction/237415

反応式

関与物質

役割名称HCID仕込み量
反応物PaclitaxelHCID 36314—
反応物Fmoc-Leu PABCHCID 131731174—
触媒4-(Dimethylamino)pyridineHCID 14284—
溶媒DichloromethaneHCID 6344—
生成物Fmoc-Leu PABC PaclitaxelHCID 13173117393%

反応手順

Paclitaxel (0.37 g, 0.44 mmol) and 4-Dimethylaminopyridine (DMAP) (0.05 g, 0.44 mmol) were added to a solution of 7 (0.27 g, 0.44 mmol) in anhydrous DCM (15 mL), and the reaction was stirred in the dark at room temperature for 24 hours. Subsequently, DCM (20 mL) was added and the reaction mixture was extracted with NaHCO3, brine and dried over sodium sulphate. The residue was purified on a silica gel column using ethyl acetate/hexane (1:1) to afford 8 (550 mg, 93%) as a white powder. ESI-MS (5 kV, MeOH): m/z (%)=1360.1 (100) [M+Na]+; HPLC (230 nm): >95%.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08642555B2
出典データセットuspto-grants-2014_02
ORD IDord-baa64055c72c46edb4b6fb547eebad34
出典メモuspto-grants-2014_02