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HRID 2094370作成日:2026年10月25日

Tetrahydrofuran → 2-(3-Tert-butoxycarbonylamino pyridin-4-yl)-5-(trifluoromethyl)benzoxazole

https://huagongshe.com/reaction/2094370

反応式

関与物質

役割名称HCID仕込み量
反応物TetrahydrofuranHCID 8028—
反応物TriphenylphosphineHCID 11776—
反応物ethyl N-ethoxycarbonyliminocarbamateHCID 220568—
反応物3-tert-butoxycarbonylamino-N-[2-hydroxy-5-(trifluoromethyl)phenyl]isonicotinamideHCID 66880252—
溶媒TolueneHCID 1140—
生成物2-(3-Tert-butoxycarbonylamino pyridin-4-yl)-5-(trifluoromethyl)benzoxazoleHCID 6687940840.6%

反応手順

To a mixture of 1.78 g of 3-tert-butoxycarbonylamino-N-[2-hydroxy-5-(trifluoromethyl)phenyl]isonicotinamide, 20 ml of tetrahydrofuran and 1.29 g of triphenylphosphine, 2.15 g of 40% toluene solution of diethyl azodicarboxylate was added dropwise at room temperature. The reaction mixture was stirred at room temperature for one hour and then stirred while heating at 50° C. for 30 minutes. The reaction mixture was cooled to room temperature, and then concentrated under reduced pressure. The residue was subjected to silica gel column chromatography to give 0.69 g of 2-(3-tert-butoxycarbonylamino pyridin-4-yl)-5-(trifluoromethyl)benzoxazole (hereinafter, referred to as “active compound 36”).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08445522B2
出典データセットuspto-grants-2013_05
ORD IDord-e991dae00ed347b19a1586f40c23e9d2
出典メモuspto-grants-2013_05