反应详情

Under a nitrogen atmosphere, 1.37 g (1.84 mmol) of 1-{4-[2-(1-methyl-1-phenyl-ethyl)-2H-tetrazol-5-yl]-phenyl}-4(S)-hydroxy-2-(tert-butoxycarbonyl)amino-5(S)-N-(N-methoxycarbonyl-(L)-tert-leucyl)amino-6-phenyl-2-azahexane are stirred in 64 ml of acetonitrile and 64 ml of aqueous 2N HCl at room temperature for 6 days. The reaction mixture is filtered, and the filtrate is concentrated by evaporation under a high vacuum at room temperature and is finally lyophilised from dioxane to yield the title compound: HPLC20-100 : tRet =14.2; 1H-NMR (CD3OD) inter alia δ 8.10 (d, J=8, 2Harom), 7.8 (m, 1Harom), 7.53 (m, 2Harom), 7.32 (m, 3Harom), 7.17 (m, 6Harom), 2.23 (s, 2H3Ctetrazole-protecting group).

1. filtrationThe reaction mixture is filtered
2. concentrationthe filtrate is concentrated by evaporation under a high vacuum at room temperature