Hydrochloric Acid → 1-amino-3-[7-(benzyloxy)-1,1-dioxido-4H-1,2,4-benzothiadiazin-3-yl]-4-hydroxyquinolin-2(1H)-one

関与物質

役割	名称	HCID	仕込み量
反応物	Hydrochloric Acid	HCID 313	—
反応物	1-amino-N-[2-(aminosulfonyl)-4-(benzyloxy)phenyl]-4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamide	HCID 67064035	—
溶媒	Potassium Hydroxide	HCID 14797	—
生成物	1-amino-3-[7-(benzyloxy)-1,1-dioxido-4H-1,2,4-benzothiadiazin-3-yl]-4-hydroxyquinolin-2(1H)-one	HCID 136358484	67.4%

反応条件

温度	125 °C

反応手順

The product of Example 304E (3.13 g, 6.51 mmol) was suspended in 10% potassium hydroxide solution (50 mL), heated at 125° C. for 24 hours then at 140° C. for 24 hours. The mixture was poured into ice and 1 M hydrochloric acid, filtered, and dried to give the title compound (2.03 g, 67%). MS (ESI−) m/z 461 (M−H)−. 1H NMR (300 MHz, DMSO-d6) δ ppm 5.18 (s, 2 H) 5.33 (s, 2 H) 7.06 (m, 1 H) 7.25 (m, 3 H) 7.43 (m, 6 H) 7.69 (d, J=7.72 Hz, 1 H) 8.06 (d, J=8.09 Hz, 1 H) 16.31 (s, 1 H).

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07902203B2
出典データセット	uspto-grants-2011_03
ORD ID	ord-c6ed92d1900f40c8a9659ddc30e54cb1
出典メモ	uspto-grants-2011_03