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HRID 472391作成日:2026年10月26日

4-(1-Methylpiperidin-4-yl)aniline → N-Methyl-N-[3-({2-[4-(1-methyl-piperidin-4-yl)-phenylamino]-[1,2,4]triazolo[1,5-a]pyridin-8-ylamino}-methyl)-pyridin-2-yl]-methanesulfonamide

https://huagongshe.com/reaction/472391

反応式

関与物質

役割名称HCID仕込み量
反応物4-(1-Methylpiperidin-4-yl)anilineHCID 21959529—
反応物2,2'-Bis(dicyclohexylphosphino)-1,1'-biphenylHCID 24946987—
反応物N-{3-[(2-Chloro-[1,2,4]triazolo[1,5-a]pyridin-8-ylamino)-methyl]-pyridin-2-yl}-N-methyl-methanesulfonamideHCID 67478948—
生成物N-Methyl-N-[3-({2-[4-(1-methyl-piperidin-4-yl)-phenylamino]-[1,2,4]triazolo[1,5-a]pyridin-8-ylamino}-methyl)-pyridin-2-yl]-methanesulfonamideHCID 49838778—

反応手順

N-Methyl-N-[3-({2-[4-(1-methyl-piperidin-4-yl)-phenylamino]-[1,2,4]triazolo[1,5-a]pyridin-8-ylamino}-methyl)-pyridin-2-yl]-methanesulfonamide was prepared from N-{3-[(2-chloro-[1,2,4]triazolo[1,5-a]pyridin-8-ylamino)-methyl]-pyridin-2-yl}-N-methyl-methanesulfonamide (75.0 mg, 0.204 mmol) and 4-(1-methyl-piperidin-4-yl)-phenylamine (47.0 mg, 0.247 mmol) with 2,2′-bis-dicyclohexylphosphanyl-biphenyl (25.0 mg, 0.0457 mmol) as the ligand in a manner analogous to Example 2d. Product isolated as a yellow foam (0.061 g, 57%). 1H NMR (400 MHz, CDCl3, δ, ppm): 8.41 (dd, J=4.7, 1.5 Hz, 1H), 7.87-7.80 (m, 2H), 7.50 (d, J=8.5 Hz, 2H), 7.29-7.25 (m, 1H), 7.20 (d, J=8.5 Hz, 2H), 6.69-6.62 (m, 2H), 6.30 (d, J=7.6 Hz, 1H), 5.29 (t, 5.8 Hz, 1H), 4.77 (d, J=6.2 Hz, 2H), 3.32 (s, 3H), 3.09 (s, 3H), 3.01-2.94 (m, 2H), 2.50-2.40 (m, 1H), 2.33 (s, 3H), 3.10-2.00 (m, 2H), 1.87-1.73 (m, 4H). MS=521 (MH)+.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08633173B2
出典データセットuspto-grants-2014_01
ORD IDord-6e45fd26c82b416b941f4c637957fd87
出典メモuspto-grants-2014_01