| 摘要 |
Prototype renin inhibitors having the general structure <IMG> where n is 0-3 inclusive, A are either both hydrogen atoms or together are a single carbon-nitrogen bond, R1 is hydrogen, or hydrocarbylcarboxy wherein the hydrocarbyl entity is selected from the group consisting of alkyl of 1 to 6 carbon atoms or aralkyl of 7 to 10 carbon atoms, R2 is an alkyl of 1 to 4 carbon atoms or cycloalkyl of 3 to 6 carbon atoms, R3 is an alkyl of 1 to 4 carbon atoms, an alkenyl of 2 to 4 carbon atoms, a phenylalkyl of 7 to 10 carbon atoms, R4 is alkyl of 1 to 6 carbon atoms or alkyl of 1 to 6 carbon atoms substituted by one or more oxygen or nitrogen containing groups, R5 is selected from aromatics, substituted aromatics and heteroaromatics, substituted or unsubstituted cycloalkyls, cycloalkenes having 3 to 8 carbon atoms, with substituents selected from alkyl, alkoxy of 3 to 10 carbon atoms, primary and secondary amides, alkyl derivatives, are prepared by novel multistep synthesis. Such compounds are valuable intermediates for the manufacture of pharmaceuticals such as Renin inhibitors and IIIV-protease inhibitors.
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