Aspirin → 2-hydroxy-N-(2-(4-(isopropylsulfonyl)phenyl)-5-trityl-5H-pyrrolo[2,3-b]pyrazin-7-yl)benzamide

関与物質

役割	名称	HCID	仕込み量
反応物	Aspirin	HCID 2244	—
反応物	4-Methylmorpholine	HCID 7972	—
反応物	O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate	HCID 2733207	—
反応物	2-(4-Isopropylsulfonylphenyl)-5-trityl-pyrrolo[2,3-b]pyrazin-7-amine	HCID 71143591	—
溶媒	Dichloromethane	HCID 6344	—
生成物	2-hydroxy-N-(2-(4-(isopropylsulfonyl)phenyl)-5-trityl-5H-pyrrolo[2,3-b]pyrazin-7-yl)benzamide	HCID 71154982	—

反応手順

A 5 mL microwave vial was charged with 2-acetoxybenzoic acid (33.87 mg, 0.1880 mmol) To this was added a solution of 2-(4-isopropylsulfonylphenyl)-5-trityl-pyrrolo[2,3-b]pyrazin-7-amine (100 mg, 0.1790 mmol), TBTU in DCM (1 mL) followed by PS-NMM. The reaction was shaken for 3 hours at ambient temperature then filtered and the resin washed with DCM (1 mL). This crude mixture was taken onto the next step as is.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US08822469B2
出典データセット	uspto-grants-2014_09
ORD ID	ord-b41611152f6444abbee94ae2e2d8366d
出典メモ	uspto-grants-2014_09