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HRID 76437作成日:2026年10月25日

2,4-Dichloro-5-fluoropyrimidine → 2-chloro-5-fluoro-N4-[2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one-6-yl]-4-pyrimidineamine

https://huagongshe.com/reaction/76437

反応式

関与物質

役割名称HCID仕込み量
反応物2,4-Dichloro-5-fluoropyrimidineHCID 250705—
反応物2-chloro-5-fluoro-N-(3,4-ethylenedioxyphenyl)-4-pyrimidineamineHCID 22060362—
反応物6-amino-2H,3H,4H-pyrido[3,2-b][1,4]oxazin-3-oneHCID 22060563—
生成物2-chloro-5-fluoro-N4-[2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one-6-yl]-4-pyrimidineamineHCID 22060403—

反応手順

In a manner similar to the preparation of 2-chloro-N4-(3,4-ethylenedioxyphenyl)-5-fluoro-4-pyrimidineamine, 2,4-dichloro-5-fluoropyrimidine and 6-amino-2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one were reacted to yield 2-chloro-5-fluoro-N4-[2H-pyrido[3,2-b]-1,4-oxazin-3(4H)-one-6-yl]-4-pyrimidineamine. 1H NMR (DMSO-d6): δ 4.63 (s, 2H), 7.34 (d, J=8.7 Hz, 1H), 7.44 (d, J=8.4 Hz, 1H), 8.33 (d, J=3.3 Hz, 1H), 10.14 (s, 1H, NH), 11.19 (s, 1H, NH); 19F NMR (282 MHz, DMSO-d6): δ −152.35; LCMS: ret. time: 26.74 min.; purity: 85.90%; MS (m/e): 296.13 (MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08835430B2
出典データセットuspto-grants-2014_09
ORD IDord-e4c0f657ea694d859686350de465e535
出典メモuspto-grants-2014_09