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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 300생성일: 2026년 10월 23일

8-Chloro-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine → N-(6-Methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine

https://huagongshe.com/ko/reaction/300

반응식

참여 물질

역할이름HCID투입량
반응물8-Chloro-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepineHCID 57512860—
반응물6-Methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-ylamineHCID 57512866—
시약Sodium t-butoxideHCID 23676156—
촉매Binap, (A+-)-HCID 634876—
촉매Bis(dibenzylideneacetone)palladiumHCID 9811564—
용매TolueneHCID 1140—
생성물N-(6-Methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amineHCID 575128269.77%

반응 조건

온도100 °C

반응 단계

6-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-amine (104 mg, 0.51 mmol), 8-chloro-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepine (150 mg, 0.51 mmol), Sodium tert-butoxide (73.4 mg, 0.76 mmol), rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (22.19 mg, 0.04 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (32.6 mg, 0.04 mmol) were added to a radley tube followed by toluene (6 mL). The reaction mixture was flushed with argon and the mixture was heated to 100°C and stirred overnight. The solids were filtered off and washed with DCM. The crude product was purified on prepHPLC yielding N-(6-methoxy-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2-yl)-4,6-dimethyl-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydropyrido[3,2-f][1,4]oxazepin-8-amine (23.00 mg, 9.77 %)

출처 및 근거

출처 데이터셋750 AstraZeneca ELN dataset
ORD IDord-916b542fdcc44d6284100092f1e92c3f
출처 메모750 AstraZeneca ELN dataset