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Potent inhibitors of HIV-protease such as 1 can be produced on a kilogram scale by diastereoselective, reductive dimerization of homochiral peptide aldehydes. This is made possible by the use of niobium catalysts or vanadium catalysts generated in situ in the crucial reaction step. aryl = 1-naphthyl.
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Kammermeier et al. (1994) studied this question.
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