Sodium Carbonate → N-[4-(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	(4-Methanesulfonamidophenyl)boronic acid	HCID 2773537	—
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-[4-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-phenyl]-methanesulfonamide	HCID 24905161	3%

反応条件

温度	80 °C

反応手順

A solution of 4-methanesulfonylaminophenylboronic acid (24 mg, 0.11 mmol) in EtOH (3.3 mL) was added to a solution of 3-iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine (30 mg, 0.10 mmol) in DME (12 mL). Pd(PPh3)4 (30 mg, 0.03 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 BA40 (0.9 mg, 3% 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	US08642604B2
出典データセット	uspto-grants-2014_02
ORD ID	ord-d158d0ef71f5469db19920c2e7ae6e2d
出典メモ	uspto-grants-2014_02