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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 410409생성일: 2026년 10월 26일

Cesium carbonate → Methyl 3-(1,3-thiazol-5-yl)-5-{[4-(trifluoromethyl)pyrimidin-2-yl]amino}benzoate

https://huagongshe.com/reaction/410409

반응식

참여 물질

역할이름HCID투입량
반응물Cesium carbonateHCID 10796—
반응물5-BromothiazoleHCID 546059—
반응물2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenylHCID 11155794—
반응물Methyl 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5-{[4-(trifluoromethyl)pyrimidin-2-yl]amino}benzoateHCID 67433486—
촉매Bis(dibenzylideneacetone)palladiumHCID 9811564—
용매WaterHCID 962—
용매1,4-DioxaneHCID 31275—
생성물Methyl 3-(1,3-thiazol-5-yl)-5-{[4-(trifluoromethyl)pyrimidin-2-yl]amino}benzoateHCID 6726214272%

반응 조건

온도90 °C

반응 단계

To a flask containing the product of Step 2 (391 mg, 0.92 mmol), dicyclohexyl[2′,4′,6′-tri(propan-2-yl)biphenyl-2-yl]phosphane (44 mg, 0.092 mmol), Pd2(dba)3 (42 mg, 0.046 mmol), cesium carbonate (602 mg, 1.85 mmol) was added a solution of 5-bromothiazole in a degassed mixture of dioxane (8.4 mL) and water (840 μL). The solution was evacuated and then purged with argon 5 times and then heated at 90° C. overnight. The reaction was cooled, diluted with ethyl acetate, washed with water, dried over magnesium sulfate, filtered and concentrated. Flash chromatography was used for purification to yield methyl 3-(1,3-thiazol-5-yl)-5-{[4-(trifluoromethyl)pyrimidin-2-yl]amino}benzoate (254 mg, 0.67 mmol, 72% yield). MS ESI: [M+H]+ m/z 381.0.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08759366B2
출처 데이터셋uspto-grants-2014_06
ORD IDord-79ed51a88cc44ae08a6a751b14a0d053
출처 메모uspto-grants-2014_06