3-Fluorophenyl isocyanate → 4-{5-[(6,7-Dichloro-1-oxo-1,2-dihydropyrrolo[1,2-a]pyrazin-4-yl)methyl]-2-fluorobenzoyl}-n-(3-fluorophenyl)piperazine-1-carboxamide

関与物質

役割	名称	HCID	仕込み量
反応物	3-Fluorophenyl isocyanate	HCID 123064	—
反応物	6,7-dichloro-4-(4-fluoro-3-(piperazine-1-carbonyl)benzyl)pyrrolo[1,2-a]pyrazin-1(2H)-one	HCID 46229754	—
溶媒	Dimethylformamide	HCID 6228	—
生成物	4-{5-[(6,7-Dichloro-1-oxo-1,2-dihydropyrrolo[1,2-a]pyrazin-4-yl)methyl]-2-fluorobenzoyl}-n-(3-fluorophenyl)piperazine-1-carboxamide	HCID 24872152	—

反応手順

To a solution of Example 16, P1 in DMF (0.1 M) was added 1-fluoro-3-isocyanatobenzene (1 eq). The resulting mixture was stirred for 1 hour at RT. The product was isolated by purification at preparative-HPLC. 1H NMR (300 MHz, DMSO-d6) δ: 10.90 (1H, m), 8.80 (1H, s), 7.48-7.37 (1H, m), 7.35-7.20 (5H, m), 7.15 (1H, s), 6.80-6.69 (1H, m), 6.55 (1H, m), 4.38 (2H, m), 3.72-3.62 (2H, m), 3.59-3.50 (2H, m), 3.44-3.35 (2H, m), 3.27-3.16 (2H, m). MS (ES) C26H21Cl2F2N5O3 requires: 559/561, found: 560/562 (M+H)+.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07834015B2
出典データセット	uspto-grants-2010_11
ORD ID	ord-8a7cafc925e54643972ee035d3f3ae70
出典メモ	uspto-grants-2010_11