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Title:
【発明の名称】5-アミノ-4-ヒドロキシ吉草酸誘導体の製造方法
Document Type and Number:
Japanese Patent JP2571230
Kind Code:
B2
Abstract:
A novel process and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula in which R<1> represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl(lower alkyl), aryl, aryl(lower alkyl) or the radical of a natural amino acid, R<2> represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl(lower alkyl), aryl, aryl(lower alkyl), amino, hydroxyl, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid and R<3> represents optionally substituted hydroxyl or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the gamma , delta -unsaturated acid obtainable or a suitable derivative thereof, replacement of halogen by a nitrogen-containing nucleophile, lactone ring-opening and liberation of the amino group. Compounds of the formula I are starting substances for the preparation of renin inhibitors having anti-hypertensive activity.

Inventors:
PEETAA HERORUTO
KURISUTOFU ANGUSUTO
Application Number:
JP20008587A
Publication Date:
January 16, 1997
Filing Date:
August 12, 1987
Export Citation:
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Assignee:
CIBA GEIGY
International Classes:
C07C27/00; C07C29/40; C07C33/12; C07C51/00; C07C51/347; C07C51/353; C07C57/00; C07C57/02; C07C57/03; C07C57/26; C07C59/42; C07C67/00; C07C67/343; C07C69/52; C07C69/527; C07C69/533; C07C69/618; C07C227/00; C07C227/06; C07C229/22; C07C229/26; C07C229/28; C07C229/34; C07C231/00; C07C231/02; C07C231/12; C07C233/00; C07C233/09; C07C233/10; C07C237/04; C07C237/06; C07C237/08; C07C237/12; C07C237/14; C07C237/16; C07C237/18; C07C239/00; C07C241/00; C07C247/12; C07C259/06; C07C313/00; C07C315/04; C07C317/44; C07C317/48; C07C319/12; C07C319/20; C07C323/58; C07C323/60; C07C401/00; C07C403/20; C07D261/02; C07D295/10; C07D295/18; C07D307/32; C07D307/33; C07F7/18; (IPC1-7): C07C237/06; C07C231/12; C07C315/04; C07C317/44; C07C319/20; C07C323/60; C07D295/10; C07D295/18
Attorney, Agent or Firm:
Aoki Akira (4 outside)



 
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