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HRID 533287作成日:2026年10月25日

Metronidazole → Metronidazole Carbonate

https://huagongshe.com/reaction/533287

反応式

関与物質

役割名称HCID仕込み量
反応物MetronidazoleHCID 4173—
反応物TriphosgeneHCID 94429—
触媒4-(Dimethylamino)pyridineHCID 14284—
溶媒DichloromethaneHCID 6344—
生成物Metronidazole CarbonateHCID 68777643356.1%

反応手順

mPEG11OH (0.39 mmol, 200 mg) and DMAP (0.93 mmol) were dissolved in anhydrous DCM (10 ml). Triphosgene (0.13 mmol, 38.5 mg) was added at room temperature. The solution was stirred at room temperature for ten minutes. Metronidazole (0.43 mmol, 73.5 mg) was added and the reaction solution was stirred at room temperature overnight. The solvent was evaporated at reduced pressure. The residue was subjected to flash chromatography (methanol/DCM=2˜5%) to obtain compound 2c (107 mg, yield 38%). 1H NMR (CDCl3) δ 7.92 (s, 1H), 4.55 (t, 2H), 4.45 (t, 2H), 4.21 (t, 2H), 3.66-3.49 (m, 42H), 3.33 (s, 3H), 2.47 (s, 3H). LC/MS 714 [M+H]+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08853247B2
出典データセットuspto-grants-2014_10
ORD IDord-98f760f30c594d7085976049b2895f87
出典メモuspto-grants-2014_10