Diethyl Ether → Ethyl 8-{[1-(tert-butoxycarbonyl)pyrrolidin-3-yl]amino}-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate

HRID 44599

반응식

HRID 44599 반응식
[CH3:1][N:2]1[C:14]2[C:13]3[N:12]=[C:11](OS(C(F)(F)F)(=O)=O)[N:10]=[CH:9][C:8]=3[CH2:7][CH2:6][C:5]=2[C:4]([C:23]([O:25][CH2:26][CH3:27])=[O:24])=[N:3]1.[NH2:28][CH:29]1[CH2:33][CH2:32][N:31]([C:34]([O:36][C:37]([CH3:40])([CH3:39])[CH3:38])=[O:35])[CH2:30]1.C(OCC)C>O1CCOCC1>[C:37]([O:36][C:34]([N:31]1[CH2:32][CH2:33][CH:29]([NH:28][C:11]2[N:10]=[CH:9][C:8]3[CH2:7][CH2:6][C:5]4[C:4]([C:23]([O:25][CH2:26][CH3:27])=[O:24])=[N:3][N:2]([CH3:1])[C:14]=4[C:13]=3[N:12]=2)[CH2:30]1)=[O:35])([CH3:40])([CH3:38])[CH3:39]

참가 물질

5

반응물 3

HCID 3283Diethyl EtherHCID 27563701-Boc-3-aminopyrrolidineHCID 45141798Ethyl 1-methyl-8-([(trifluoromethyl)sulfonyl]oxy}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate

생성물 1

HCID 57444099Ethyl 8-{[1-(tert-butoxycarbonyl)pyrrolidin-3-yl]amino}-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate수율 88%

시약·촉매·용매 1

HCID 312751,4-Dioxane용매

실험 절차

To a solution of 1.5 g (3.7 mmol) of ethyl 1-methyl-8-{[(trifluoromethyl)sulfonyl]oxy}-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylate in 150 mL of anhydrous dioxane, 756 mg (4.1 mmol) of tert-butyl 3-aminopyrrolidine-1-carboxylate were added. The reaction mixture was stirred at room temperature overnight. The solvent was then removed under reduced pressure, the residue redissolved with dichloromethane and washed with water. The organic layer was dried over sodium sulfate and evaporated. 1.2 g (88% yield) of the title compound was collected by filtration after trituration with diethylether.

후처리

  1. customThe solvent was then removed under reduced pressure
  2. dissolutionthe residue redissolved with dichloromethane
  3. washwashed with water
  4. dry with materialThe organic layer was dried over sodium sulfate
  5. customevaporated

출처 및 근거

ORD 기록
ord-20e3214f3f9f43fb9433b77ede651b0f
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08541429B2

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