Key result
Highly active renin inhibitors containing N-terminal sulfonemethylene and C-terminal hydroxyethylene isosteres were efficiently synthesized via a stereospecific key intermediate.
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May enable new renin inhibitors for hypertension; leaves open clinical translation and efficacy testing.
We describe an efficient synthesis of highly active renin inhibitors containing a sulfonemethylene isostere at their N-terminals and a hydroxyethylene isostere at their C-terminals. The stereospecific synthesis of N-terminal key intermediate, L-N-[(2R)-2-benzyl(or 1-naphthylmethyl)-3-hydroxypropionyl]norleucine t-butyl ester is described.
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Nakano et al. (1990) studied this question. Highly active renin inhibitors containing N-terminal sulfonemethylene and C-terminal hydroxyethylene isosteres were efficiently synthesized via a stereospecific key intermediate.
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