以(2S,3S)-1,2-环氧基-3-叔丁氧酰胺基4-苯丁烷为原料,经过异丁基胺化、N-对硝基苯磺酰化、还原、脱保护后再与(S)-3-羟基四氢呋喃-琥珀酰亚胺基碳酸酯(7)缩合制得安普那韦,总收率73%,其结构经^1H NMR和MS确证。
Amprenavir in overall yield of 73% was obtained from (2S,3S)-3-(t-butoxy)-amido-1,2- epoxy-4-phenylbutane via isobutylamination, N-4-nitrobenzene sulfonylation, reduction, deprotection, and then condensation with 7. The structure was confirmed by ^1H NMR and MS.