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HRID 347772作成日:2026年10月26日

Sodium Carbonate → 5-(2-chlorophenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-3-[2(R)-amino-2-phenylethyl]-pyrimidine-2,4(1H,3H)-dione

https://huagongshe.com/reaction/347772

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物2-Chlorophenylboronic acidHCID 2734322—
反応物5-bromo-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-3-[2(R)-amino-2-phenylethyl]-pyrimidine-2,4(1H,3H)-dioneHCID 21027676—
触媒HCID 178418397HCID 178418397—
溶媒1,4-Dioxane--water (1/1)HCID 21886435—
生成物5-(2-chlorophenyl)-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methyl-3-[2(R)-amino-2-phenylethyl]-pyrimidine-2,4(1H,3H)-dioneHCID 21027675—

反応条件

温度90 °C

反応手順

To compound 2a (40 mg, 0.08 mmol) in 0.25 mL/0.75 mL of H2O/dioxane in a 4 mL vial was added 2-chlorophenyl boronic acid (0.12 mmol) and sodium carbonate (51 mg, 0.48 mmol, 6 eq). Nitrogen gas was bubbled through the solution for 1 minute and tetrakis(triphenylphosphine)palladium (9.24 mg, 0.008 mmol) was added. The resulting mixture was sealed and heated at 90° C. overnight. After cooling to ambient temperature, the precipitate was removed by filtration and was purified by prep. LC-MS to give 2b.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07176211B2
出典データセットuspto-grants-2007_02
ORD IDord-6f15e5fe9bb54f9eb94c0375497b766f
出典メモuspto-grants-2007_02