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HRID 13031作成日:2026年10月26日

Ethyl trifluoroacetate → N-[(1R,2S)-1-[4-(ethylsulfanylmethyl)phenyl]-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-propan-2-yl]-2,2,2-trifluoro-acetamide

https://huagongshe.com/reaction/13031

反応式

関与物質

役割名称HCID仕込み量
反応物Ethyl trifluoroacetateHCID 9794—
反応物1,1,3,3-TetramethylguanidineHCID 66460—
反応物(1R,2S)-1-(4-(ethylthiomethyl)phenyl)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)propan-2-amine hydrochlorideHCID 66812805—
溶媒MethanolHCID 887—
生成物N-[(1R,2S)-1-[4-(ethylsulfanylmethyl)phenyl]-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-propan-2-yl]-2,2,2-trifluoro-acetamideHCID 25013993—

反応手順

(1R,2S)-1-(4-(ethylthiomethyl)phenyl)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)propan-2-amine hydrochloride (50 mg, 0.11 mmol), 1,1,3,3-tetramethylguanidine (100 μl, 0.79 mmol) and ethyl trifluoroacetate (200 μl, 1.68 mmol) in MeOH (2.5 mL) was stirred at r.t. for 1 h. The reaction mixture was concentrated by evaporation and the residual material was purified by HPLC. Yield 35 mg (62%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07728030B2
出典データセットuspto-grants-2010_06
ORD IDord-a2252fd42a3f43c4a7f1ff961adb5d8b
出典メモuspto-grants-2010_06