Ammonia → N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-naphthalen-2-yl-propan-2-yl]-2-hydroxy-acetamide

関与物質

役割	名称	HCID	仕込み量
反応物	Ammonia	HCID 222	—
反応物	Acetoxyacetyl chloride	HCID 26297	—
反応物	Diisopropylethylamine	HCID 81531	—
反応物	(1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)-1-(naphthalen-2-yl)propan-2-amine hydrochloride	HCID 66812502	—
溶媒	Methanol	HCID 887	—
溶媒	Water	HCID 962	—
溶媒	Tetrahydrofuran	HCID 8028	—
生成物	N-[(1R,2S)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-1-naphthalen-2-yl-propan-2-yl]-2-hydroxy-acetamide	HCID 25013813	—

反応手順

Acetoxyacetyl chloride (13 μL, 0.12 mmol) was added to a stirred mixture of (1R,2S)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)-1-(naphthalen-2-yl)propan-2-amine hydrochloride (20a) (50 mg, 0.11 mmol) and N,N-diisopropylethylamine (60 μL, 0.34 mmol) in THF (2 mL). The reaction mixture was stirred at r.t. 45 min. Water (0.5 mL), 28% (aq) NH3 (0.5 mL) and MeOH (0.5 mL) was added to give a clear one-phase solution, the mixture was stirred over night at r.t.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07728030B2
出典データセット	uspto-grants-2010_06
ORD ID	ord-50fee426e9f84e2e8afe7b5b6f30eda3
出典メモ	uspto-grants-2010_06