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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 57445생성일: 2026년 10월 24일

Potassium Carbonate → (R)-N-((S)-1-(2,5-difluoro-4-(2-(trifluoromethyl)pyridin-4-yl)phenyl)ethyl)-2-methylpropane-2-sulfinamide

https://huagongshe.com/ko/reaction/57445

반응식

참여 물질

역할이름HCID투입량
반응물Potassium CarbonateHCID 11430—
반응물Sodium 2'-(dicyclohexylphosphino)-2,6-dimethoxybiphenyl-3-sulfonateHCID 23677046—
반응물2-(Trifluoromethyl)pyridine-4-boronic acidHCID 45158880—
반응물(R)-N-((S)-1-(4-bromo-2,5-difluorophenyl)ethyl)-2-methylpropane-2-sulfinamideHCID 90347558—
촉매Bis(dibenzylideneacetone)palladiumHCID 9811564—
용매WaterHCID 962—
용매Ethyl AcetateHCID 8857—
용매1,4-Dioxane--water (1/1)HCID 21886435—
생성물(R)-N-((S)-1-(2,5-difluoro-4-(2-(trifluoromethyl)pyridin-4-yl)phenyl)ethyl)-2-methylpropane-2-sulfinamideHCID 90414875—

반응 조건

온도110 °C

반응 단계

To a solution of (R)—N—((S)-1-(4-bromo-2,5-difluorophenyl)ethyl)-2-methylpropane-2-sulfinamide (230 mg, 0.676 mmol) in dioxane/H2O (5 mL/1 mL) was added sodium 2′-(dicyclohexylphosphino)-2,6-dimethoxy-[1,1′-biphenyl]-3-sulfonate (34.7 mg, 0.068 mmol), (2-(trifluoromethyl)pyridin-4-yl)boronic acid (194 mg, 1.014 mmol), K2CO3 (234 mg, 1.690 mmol) followed by Pd2dba3 (31.0 mg, 0.034 mmol). The reaction mixture was sealed and heated to 110° C. and stirred for 2 hours. LCMS show complete conversion. The reaction mixture was then cooled to room temperature and diluted with EtOAc (20 mL) and water (10 mL). The aqueous layer was then extracted with EtOAc (2×20 mL). The combined organic was then concentrated. The residue was purified by silica gel chromatography (50% heptane in EtOAc to 10% MeOH in EtOAc) to give product. (0.25 g). LCMS (B) m/z 407.6 (M+H)+

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US09434719B2
출처 데이터셋uspto-grants-2016_09
ORD IDord-96026f0949044e428cd32fdaf51b7e0a
출처 메모uspto-grants-2016_09