Processes for the preparation of 5-amino-4-hydroxy

专利名称：Processes for the preparation of 5-amino-4-hydroxyvaleric acid derivatives

发明人：Peter Herold,Christof Angst申请号：US07/0837申请日：19870813公开号：US0477A公开日：19900206

摘要：The invention relates to novel processes and intermediates for the preparationof 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl,aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen,optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl,amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, andR.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic

rearrangement of a suitable allyl ester, halolactonisation of the resulting &ggr;,&dgr;-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group.Compounds of the formula I are starting materials for the preparation of renin-inhibitorswhich have an anti-hypertensive action.

申请人：CIBA-GEIGY CORPORATION

代理人：JoAnn Villamizar,Irving M. Fishman

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