| 摘要 |
A process for the preparation of hydroxy lactone of the Formula (CVI) comprising (i) contacting a salt of the Formula (CIV) with an acid to produce a free acid, (2) extracting the free acid from the reaction mixture, (3) contacting the free acid with an activating agent, (4) contacting the reaction mixture of free acid/activating agent with malonate monoester and a divalent metal, (5) contacting the reaction mixture of step (4) with an acid, (6) contacting the reaction mixture of step (5) with a base in the presence of a C1-4alcohol, THF or DMF. The compound [R-(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (XIX) is a protease inhibitor useful in treating humans infected with the HIV virus. Wherein; R1 is C1-6alkyl, cyclohexyl, phenyl, -CH2CH2-FR1-1 wherein R1-1 is -OH, -NH2, -H, -NH-CO-CH3, N(-CO-CH3)2; R2 is C1-6alkyl, cyclohexyl, phenyl, -CH2-CH2-FR2-1, wherein R2-1 is -OH, -NH2, -H, -NH-CO-CH3, N(-CO-CH3)2.
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