반응 #42800

반응 방정식

4-chloro-5-fluoro-6-(2-pentynyloxy)pyrimidine

3,5-dimethylpiperidine

→

4-(3,5-dimethylpiperidino)-5-fluoro-6-(2-pentynyloxy)pyrimidine

수율 84.7%

반응 조건

실험 절차

0.2 g of 4-chloro-5-fluoro-6-(2-pentynyloxy)pyrimidine and 0.32 g of 3,5-dimethylpiperidine (cis/trans=about 3/1) were mixed and left for 3 hours at room temperature. The reaction mixture was subjected to silica gel column chromatography to obtain 0.23 g of 4-(3,5-dimethylpiperidino)-5-fluoro-6-(2-pentynyloxy)pyrimidine (hereinafter, referred to as Compound (11)). Compound (11) had the cis/trans diastereomer originated two methyls on the piperidine ring. The ratio of the cis/trans diastereomer was about 3.8/1.

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