Water → N-tert-butyl-2-(1-(2-(2,2-dimethyl-1,3-dioxolan-4-yl)ethyl)-6-fluoro-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxamide

関与物質

役割	名称	HCID	仕込み量
反応物	Water	HCID 962	—
反応物	Potassium Carbonate	HCID 11430	—
反応物	2-(2,2-Dimethyl-1,3-dioxolan-4-yl)ethyl methanesulfonate	HCID 13194536	—
反応物	N-tert-butyl-2-(6-fluoro-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxamide	HCID 71280404	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	N-tert-butyl-2-(1-(2-(2,2-dimethyl-1,3-dioxolan-4-yl)ethyl)-6-fluoro-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxamide	HCID 71279519	92.2%

反応条件

温度	65 °C

反応手順

To a solution of N-tert-butyl-2-(6-fluoro-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxamide (80 mg, 0.135 mmol) in DMF (5 mL) was added 2-(2,2-dimethyl-1,3-dioxolan-4-yl)ethyl methanesulfonate (36 mg, 0.162 mmol) followed by K2CO3 (56 mg, 0.405 mmol). The mixture was heated at 65° C. for 4 hours. After cooling to room temperature, the mixture was poured into water, filtered and dried to give N-tert-butyl-2-(1-(2-(2,2-dimethyl-1,3-dioxolan-4-yl)ethyl)-6-fluoro-1H-indazol-3-yl)-5-trityl-5H-pyrrolo[3,2-b]pyrazine-7-carboxamide (90 mg, 92%) The crude was used to the next step without purification. LCMS: (M+H)+=723.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08658646B2
出典データセット	uspto-grants-2014_02
ORD ID	ord-1a60e12ea4934a9791b56a3be01fdbe8
出典メモ	uspto-grants-2014_02