Potassium Phosphate, Tribasic → 1-(4-Cyclopropylpyridin-3-yl)-3-(2-(trifluoromethyl) pyridin-4-yl)imidazolidin-2-one

HRID 523529

반응식

HRID 523529 반응식
[CH:1]1([C:4]2[CH:9]=[CH:8][N:7]=[CH:6][C:5]=2[N:10]2[CH2:14][CH2:13][NH:12][C:11]2=[O:15])[CH2:3][CH2:2]1.Br[C:17]1[CH:22]=[CH:21][N:20]=[C:19]([C:23]([F:26])([F:25])[F:24])[CH:18]=1.CN[C@@H]1CCCC[C@H]1NC.P([O-])([O-])([O-])=O.[K+].[K+].[K+]>[Cu](I)I>[CH:1]1([C:4]2[CH:9]=[CH:8][N:7]=[CH:6][C:5]=2[N:10]2[CH2:14][CH2:13][N:12]([C:17]3[CH:22]=[CH:21][N:20]=[C:19]([C:23]([F:26])([F:25])[F:24])[CH:18]=3)[C:11]2=[O:15])[CH2:3][CH2:2]1

참가 물질

6

반응물 4

HCID 62657Potassium Phosphate, TribasicHCID 2733821trans-N,N'-dimethyl-1,2-cyclohexanediamineHCID 234369504-Bromo-2-(trifluoromethyl)pyridineHCID 709820071-(4-Cyclopropylpyridin-3-yl)imidazolidin-2-one

생성물 1

HCID 665764111-(4-Cyclopropylpyridin-3-yl)-3-(2-(trifluoromethyl) pyridin-4-yl)imidazolidin-2-one수율 33.4%

시약·촉매·용매 1

HCID 83717Copper iodide촉매

실험 절차

Using analogous reagents and reaction conditions as described in Example 1 above, 1-(4-cyclopropylpyridin-3-yl)imidazolidin-2-one (I-1d: 70 mg, 0.344 mmol) was reacted with 4-bromo-2-(trifluoromethyl)pyridine (93.5 mg, 0.413 mmol) 1,4-dioxane (5 mL), copper iodide (6.5 mg, 0.034 mmol), trans-N,N′-dimethylcyclohexane-1,2-diamine (4.8 mg, 0.034 mmol) and potassium phosphate (219 mg, 1.034 mmol) to afford the crude product. Purification by preparative HPLC afforded 40 mg of the product (33% yield).

후처리

  1. customreagents and reaction conditions
  2. customto afford the crude product
  3. customPurification by preparative HPLC

출처 및 근거

ORD 기록
ord-19164e7684f94acea92549cc8bbef80f
출처 데이터셋
uspto-grants-2016_05
특허 번호
US09339501B2

연결된 노트

불러오는 중…