合成路线图解说明: The reduction of 6-(4,6-diphenylpyridin-2-yloxy)-2,2-dimethylhexanenitrile (I) (J Med Chem 1992, 35: 4315) with NaBH4/TFA in THF gives 6-(4,6-diphenylpyridin-2-yloxy)-2,2-dimethylhexylamine (II), which is condensed with protected aspartic acid activated as succinimidyl ester (III) and triethylamine in DMF yielding te proteted aspartic acid amide (IV). The deprotection of (IV) with trifluoroacetic acid affords unprotected aspartamide (V), which is finally condensed with pyridine-3-carboxylic acid succinimidyl ester (VI) by means of triethylamine in DMF. |