반응 #2180475

반응 방정식

4,5-dichloro-6-(trifluoromethyl)pyrimidin-2-amine

(1R,2S)-2,6-dimethyl-2,3-dihydro-1H-inden-1-amine

potassium carbonate

→

5-chloro-N4-[(1R,2S)-2,6-dimethyl-2,3-dihydro-1H-inden-1-yl]-6-(trifluoromethyl)pyrimidin-2,4-diamine

수율 58.0%

용매

dimethylacetamide

반응 조건

후처리

1. 1
   기타The crude mixture is absorbed on silica gel
2. 2
   기타column chromatographic separation

실험 절차

A mixture of 0.10 g (0.43 mmol) of 4,5-dichloro-6-(trifluoromethyl)pyrimidin-2-amine, 0.08 g (0.51 mmol) of (1R,2S)-2,6-dimethyl-2,3-dihydro-1H-inden-1-amine and 0.14 g (1.3 mmol) of potassium carbonate in 1 ml of dimethylacetamide as solvent is heated at 125° C. for 30 minutes in a microwave appliance (Biotage Initiator, http://www.biotage.com/DynPage.aspx?id=22001). The crude mixture is absorbed on silica gel and, following column chromatographic separation, 0.089 g of 5-chloro-N4-[(1R,2S)-2,6-dimethyl-2,3-dihydro-1H-inden-1-yl]-6-(trifluoromethyl)pyrimidin-2,4-diamine is obtained (solid, 55% yield, 95% purity).

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