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HRID 2370534作成日:2026年10月26日

Diisopropylethylamine → (S)-tert-butyl 3-(6-(2-chloropyridin-4-yloxy)benzo[d]thiazol-2-ylamino)piperidine-1-carboxylate

https://huagongshe.com/reaction/2370534

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物tert-butyl (3S)-3-aminopiperidine-1-carboxylateHCID 1501975—
反応物6-(2-Chloropyridin-4-yloxy)-2-(methylsulfinyl)benzo[d]thiazoleHCID 57725430—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物(S)-tert-butyl 3-(6-(2-chloropyridin-4-yloxy)benzo[d]thiazol-2-ylamino)piperidine-1-carboxylateHCID 57725807112%

反応条件

温度95 °C

反応手順

To the solution of 6-(2-chloropyridin-4-yloxy)-2-(methylsulfinyl)benzo[d]thiazole (100 mg, 0.31 mmol) in 1.6 ml of NMP was added (S)-tert-butyl 3-aminopiperidine-1-carboxylate (200 mg, 1 mmol) and DIPEA (70 μL, 0.4 mmol). The reaction solution was stirred at 95° C. for 5 days. The crude reaction solution was purified on prep HPLC and evaporated in vaccuo to give (S)-tert-butyl 3-(6-(2-chloropyridin-4-yloxy)benzo[d]thiazol-2-ylamino)piperidine-1-carboxylate (160 mg) as TFA salt. ES/MS m/z 461.1 (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-54e39376a176469aa5db12fd22dbd2de
出典メモuspto-grants-2014_04