The application discloses a preparation method of high-purity Fmoc-S-trityl-L-
penicillamine and belongs to the field of synthetic
chemistry. The method is characterized in that L-
penicillamine is used as a starting material, dehydrated with methyl
boronic acid to generate a cyclic protective structure, then a
thiol group is selectively protected by trityl, and an acid is used to open a ring to obtain an S-trityl-L-
penicillamine intermediate; then, in a
sodium bicarbonate buffered water / dioxane weak alkaline
system, Fmoc-OSu (9-fluorenylmethoxycarbonyl succinimidyl ester) is used to react with the S-trityl-L-penicillamine intermediate to protect an amino group, and
racemization is effectively inhibited; finally, the product is refined by recrystallization in an
ethyl acetate / n-
heptane system to obtain a high-purity end product. The process
route is simple and efficient, the conditions are mild, the purification method is unique and effective, the obtained product has high
chemical purity and optical purity, good stability, is suitable for large-scale production, and can meet the needs of high-end polypeptide
drug synthesis.