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HRID 2370568作成日:2026年10月26日

2-[2-(4-Methylpiperazin-1-yl)ethoxy]aniline → N-methyl-4-(2-(2-(2-(4-methylpiperazin-1-yl)ethoxy)phenylamino)benzo[d]thiazol-6-yloxy)picolinamide

https://huagongshe.com/reaction/2370568

反応式

関与物質

役割名称HCID仕込み量
反応物2-[2-(4-Methylpiperazin-1-yl)ethoxy]anilineHCID 23008788—
反応物2-Pyridinecarboxamide, N-methyl-4-[[2-(methylsulfinyl)-6-benzothiazolyl]oxy]-HCID 57725393—
溶媒Hydrochloric AcidHCID 313—
溶媒IsopropanolHCID 3776—
生成物N-methyl-4-(2-(2-(2-(4-methylpiperazin-1-yl)ethoxy)phenylamino)benzo[d]thiazol-6-yloxy)picolinamideHCID 57725420—

反応条件

温度80 °C

反応手順

To the solution of N-methyl-4-(2-(methylsulfinyl)benzo[d]thiazol-6-yloxy)picolinamide (25 mg, 0.072 mmol, 1.0 eq) in 1 mL of IPA and 1 mL conc. HCl was added 2-(2-(4-methylpiperazin-1-yl)ethoxy) aniline (25 mg, 0.108 mmol, 1.5 eq) and reaction mixture heated at 80° C. in oil bath for 2 hours. Thereafter, the product was purified via reverse phase HPLC. This procedure was generalized for other analogues for which progress of the reaction was monitored by LC-MS and amount of aniline and reaction time adjusted as needed. LC/MS (m/z) [519.1] (MH+)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08710048B2
出典データセットuspto-grants-2014_04
ORD IDord-15936e34814449d49671021b09d6a5d4
出典メモuspto-grants-2014_04