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HRID 1895738作成日:2026年10月25日

1-(tert-Butoxycarbonyl)-4-(methanesulfonyloxy)piperidine → Tert-butyl 4-(5-chloro-1-(4-(methylsulfonyl)phenyl)-2-oxo-1,2-dihydropyridin-4-yloxy)piperidine-1-carboxylate

https://huagongshe.com/reaction/1895738

反応式

関与物質

役割名称HCID仕込み量
反応物1-(tert-Butoxycarbonyl)-4-(methanesulfonyloxy)piperidineHCID 4184869—
反応物4-Hydroxy-1-(4-(methylsulfonyl)phenyl)-6-oxo-1,6-dihydropyridine-3-carbonitrileHCID 67368768—
反応物1-(5-Cyclopropylpyrimidin-2-yl)piperidin-4-yl methanesulfonateHCID 86626268—
反応物2-(5-chloro-4-hydroxy-2-oxopyridin-1(2H)-yl)-5-(methylsulfonyl)benzene-1-yliumHCID 86626269—
生成物Tert-butyl 4-(5-chloro-1-(4-(methylsulfonyl)phenyl)-2-oxo-1,2-dihydropyridin-4-yloxy)piperidine-1-carboxylateHCID 57468441—

反応手順

Example 226 was prepared according to the procedures described in Example 221 substituting tert-butyl 4-(methylsulfonyloxy)piperidine-1-carboxylate for 1-(5-cyclopropylpyrimidin-2-yl)piperidin-4-yl methanesulfonate, 2-(5-chloro-4-hydroxy-2-oxopyridin-1(2H)-yl)-5-(methylsulfonyl)benzene-1-ylium for 4-hydroxy-1-(4-(methylsulfonyl)phenyl)-6-oxo-1,6-dihydropyridine-3-carbonitrile in Step B. 1H NMR (500 MHz, CDCl3) δ ppm 8.07 (d, J=8.25 Hz, 2 H), 7.61 (d, J=8.80 Hz, 2 H), 7.42 (s, 1 H), 6.03 (s, 1 H), 4.52-4.68 (m, 1 H), 3.57-3.73 (m, 2 H), 3.40-3.56 (m, 2 H), 3.08 (s, 3 H), 1.76-2.02 (m, 4 H), 1.46 (s, 9 H). MS (ESI) 482 (M+H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08513424B2
出典データセットuspto-grants-2013_08
ORD IDord-33bac37d6cd94c4c8f9daf666e1b1173
出典メモuspto-grants-2013_08