Ethyl 4-piperidinecarboxylate → 1-(4-Pyrimidinyl)-4-(ethoxycarbonyl)piperidine

반응식

Cl.Cl[C:3]1[CH:8]=[CH:7][N:6]=[CH:5][N:4]=1.[NH:9]1[CH2:14][CH2:13][CH:12]([C:15]([O:17][CH2:18][CH3:19])=[O:16])[CH2:11][CH2:10]1>>[N:6]1[CH:7]=[CH:8][C:3]([N:9]2[CH2:14][CH2:13][CH:12]([C:15]([O:17][CH2:18][CH3:19])=[O:16])[CH2:11][CH2:10]2)=[N:4][CH:5]=1

참가 물질

반응물 2

HCID 70770Ethyl 4-piperidinecarboxylate

HCID 219225564-Chloropyrimidine hydrochloride

생성물 1

HCID 227219571-(4-Pyrimidinyl)-4-(ethoxycarbonyl)piperidine수율 46%

실험 절차

4-Chloropyrimidine hydrochloride was reacted with ethyl piperidine-4-carboxylate to give ethyl 1-(4-pyrimidinyl)piperidine-4-carboxylate in 46% yield. A mixture of the material so obtained (0.5 g), 2N aqueous hydrochloric acid (5 ml) and THF (15 ml) was stirred and heated to reflux for 18 hours. The mixture was evaporated and the residue was washed with ethyl acetate. There was thus obtained 1-(4-pyrimidinyl)piperidine-4-carboxylic acid hydrochloride salt (0.49 g, 95%);

출처 및 근거

ORD 기록: ord-898d5a453c944cdc8d5ce938a58e53ac
출처 데이터셋: uspto-grants-2000_07
DOI: 10.6084/m9.figshare.5104873.v1
특허 번호: US06090813

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