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HRID 605287作成日:2026年10月27日

5-Amino-2-methylphenol → N-(3-Dimethylamino-phenyl)-4-(4-methoxy-phenylsulfanyl)-3-(pyrido[2,3-d]pyrimidin-4-ylamino)-benzamide

https://huagongshe.com/reaction/605287

反応式

関与物質

役割名称HCID仕込み量
反応物5-Amino-2-methylphenolHCID 17818—
反応物N,N-dimethyl-m-phenylenediamineHCID 76084—
反応物3-(7-Isopropyl-pyrido[2,3-d]pyrimidin-4-ylamino)-4-(4-methoxy-phenylsulfanyl)-benzoyl chlorideHCID 86615550—
反応物4-(4-Methoxy-phenylsulfanyl)-3-(pyrido[2,3-d]pyrimidin-4-ylamino)-benzoyl chlorideHCID 86615561—
溶媒MethanolHCID 887—
生成物N-(3-Dimethylamino-phenyl)-4-(4-methoxy-phenylsulfanyl)-3-(pyrido[2,3-d]pyrimidin-4-ylamino)-benzamideHCID 67040446—

反応手順

The product from Example 260B was reacted with N,N-dimethyl-1,3-phenylenediamine according to the procedure from Example 137C substituting N,N-dimethyl-1,3-phenylenediamine for 5-amino-o-cresol and substituting the product from Example 260B for the product from Example 137B to provide the title compound as an off white solid after trituration of the reaction product from methanol (45 mg, 52%). 1H NMR (300 MHz, DMSO-D6) δ ppm: 10.33 (s, 1 H), 9.99 (s, 1 H), 9.11 (dd, J=4.41, 1.84 Hz, 1 H), 8.96 (dd, J=8.46, 1.84 Hz, 1 H), 8.63 (s, 1 H), 8.01 (d, J=1.84 Hz, 1 H), 7.82 (dd, J=8.46, 1.84 Hz, 1 H), 7.70 (dd, J=8.09, 4.41 Hz, 1 H), 7.36-7.43 (m, 2 H), 7.10-7.20 (m, 3 H), 6.97-7.04 (m, 3 H), 6.48 (td, J=4.50, 2.39 Hz, 1 H), 3.77 (s, 3 H), 2.88 (s, 6 H); MS (ESI+) m/z 523.5 (M+H)−, (ESI−) m/z 521.2 (M−H)−.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07910595B2
出典データセットuspto-grants-2011_03
ORD IDord-ff6af424ed37488389c031e7017724a0
出典メモuspto-grants-2011_03