Sodium Carbonate → N-[3-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-phenyl]-methanesulfonamide

関与物質

役割	名称	HCID	仕込み量
反応物	Sodium Carbonate	HCID 10340	—
反応物	3-Methylsulfonylaminophenylboronic acid	HCID 2773535	—
反応物	3-iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine	HCID 24905337	—
触媒	HCID 178418397	HCID 178418397	—
溶媒	Ethanol	HCID 702	—
溶媒	1,2-Dimethoxyethane	HCID 8071	—
生成物	N-[3-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-phenyl]-methanesulfonamide	HCID 24905159	54%

反応条件

温度	80 °C

反応手順

A solution of 3-Methanesulfonylaminophenylboronic acid (32 mg, 0.15 mmol) in EtOH (3.3 ml) was added to a solution of 3-iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine (40 mg, 0.13 mmol) in DME (12 ml). Pd(PPh3)4 (16 mg, 0.014 mmol) and saturated Na2CO3 (1.9 ml) were added and the reaction was heated to 80° C. under an argon atmosphere overnight. After cooling, the reaction was extracted with saturated NaCl and CH2Cl2. Organic phases were combined, concentrated in vacuo and purified by RP-HPLC (MeCN:H2O:0.1% TFA) to yield BA38 (24.3 mg, 54% yield). ESI-MS (M+H)+ m/z calcd 347.1, found 347.0.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07585868B2
出典データセット	uspto-grants-2009_09
ORD ID	ord-4c482c97cfb742e98531512d97eaeeee
出典メモ	uspto-grants-2009_09