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HRID 2374910作成日:2026年10月25日

1H-1,2,4-Triazole → 7-(1,3-benzodioxol-5-yl)-5-methyl-N-(3,4,5-trimethoxy-phenyl)imidazo[5,1-f][1,2,4]triazin-2-amine

https://huagongshe.com/reaction/2374910

反応式

関与物質

役割名称HCID仕込み量
反応物1H-1,2,4-TriazoleHCID 9257—
反応物Phosphorus oxychlorideHCID 24813—
反応物N-(1-{3-[(3,4,5-trimethoxyphenyl)amino]-1,2,4-triazin-6-yl}ethyl)-1,3-benzodioxole-5-carboxamideHCID 58712003—
溶媒PyridineHCID 1049—
生成物7-(1,3-benzodioxol-5-yl)-5-methyl-N-(3,4,5-trimethoxy-phenyl)imidazo[5,1-f][1,2,4]triazin-2-amineHCID 1148736643%

反応手順

In a similar manner as described for Example 9, N-(1-{3-[(3,4,5-trimethoxyphenyl)amino]-1,2,4-triazin-6-yl}ethyl)-1,3-benzodioxole-5-carboxamide (Intermediate 29) (61 mg, 0.134 mmol), and 1,2,4-triazole (55 mg, 0.80 mmol) in pyridine (2 mL) and phosphorous oxychloride (0.037 mL, 0.40 mmol) gave 7-(1,3-benzodioxol-5-yl)-5-methyl-N-(3,4,5-trimethoxy-phenyl)imidazo[5,1-f][1,2,4]triazin-2-amine (25 mg, 43%) as a yellow solid. 1H NMR (CD3OD): δ8.99 (s, 1H), 7.87 (s, 1H), 7.84 (d, J=1.65 Hz, 1H), 7.04 (s, 2H), 6.95 (d, J=7.87 Hz, 1H), 6.04 (s, 2H), 3.80 (s, 6H), 3.74 (s, 3H), 2.56 (s, 3H). MS m/z 435 (M+1).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07462614B2
出典データセットuspto-grants-2008_12
ORD IDord-8a77c41cc2144c1f907af4e81224ae27
出典メモuspto-grants-2008_12