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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 333859생성일: 2026년 10월 26일

Pyridine → 5-{2-[2-Chloro-4-(4-fluoro-3-methoxy-phenoxy)-phenyl]-1-hydroxy-1-trifluoromethyl-propyl}-1-methyl-1H-pyridin-2-one

https://huagongshe.com/reaction/333859

반응식

참여 물질

역할이름HCID투입량
반응물PyridineHCID 1049—
반응물(4-Fluoro-3-methoxyphenyl)boronic acidHCID 44558185—
반응물5-[2-(2-Chloro-4-hydroxy-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-1-methyl-1H-pyridin-2-oneHCID 57421314—
촉매Cupric acetateHCID 8895—
용매DichloromethaneHCID 6344—
생성물5-{2-[2-Chloro-4-(4-fluoro-3-methoxy-phenoxy)-phenyl]-1-hydroxy-1-trifluoromethyl-propyl}-1-methyl-1H-pyridin-2-oneHCID 5742131651.7%

반응 단계

To a solution of 5-[2-(2-chloro-4-hydroxy-phenyl)-1-hydroxy-1-trifluoromethyl-propyl]-1-methyl-1H-pyridin-2-one (Example 196, 200 mg) in CH2Cl2 (4 ml) were added 4-fluoro-3-methoxyphenylboronic acid (282 mg), copper-(II)-acetate (307 mg), molecular sieve and pyridine (219 mg). The mixture was stirred at room temperature under an air atmosphere with exclusion of moisture for 7 days. The mixture was filtered, diluted with CH2Cl2 and washed with 1M aqueous HCl. The organic phase was dried (MgSO4), filtered and concentrated to dryness. The product was purified by chromatography (SiO2, cyclohexane/EtOAc 1:0=>0:1) to give the title compound (139 mg) as an off-white solid. MS (m/e)=486.3 [M+H+].

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08883786B2
출처 데이터셋uspto-grants-2014_11
ORD IDord-1022c9cfb3b3434f9a2212bd4e65af53
출처 메모uspto-grants-2014_11