Synthesis of renin inhibitors containing a sulfonemethylene isostere at their N-terminals.

…, S Atsuumi, Y Koike, S Tanaka, H Funabashi…

Index: Nakano, Masato; Atsuumi, Shugo; Koike, Yutaka; Tanaka, Seiichi; Funabashi, Hiroshi; et al. Chemistry Letters, 1990 , # 4 p. 505 - 508

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Citation Number: 7

Abstract

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, LN-[(2R)-2-benzyl (or 1-naphthylmethyl)-3-hydroxypropionyl] norleucine t-butyl ester is described.