Chemistry of carbon compounds – Miscellaneous organic carbon compounds – C-metal
Patent
1974-05-28
1976-01-13
Rush, Raymond V.
Chemistry of carbon compounds
Miscellaneous organic carbon compounds
C-metal
260999, C07D26104
Patent
active
039324397
ABSTRACT:
Stabilized cycloserine compositions, having enhanced stability, and effective in releasing cycloserine compounds in vivo, are prepared by reacting D-4-amino-3-isoxazolidinone or its 5-methyl derivative with 2,4-pentanedione or alkyl-substituted-2,4-pentanedione to form the corresponding N-substituted-cycloserine compound in which one of the hydrogens attached to the primary amino group is replaced by 1-methyl-3-oxo-1-butenyl or an alkyl substituted-1-methyl-3-oxo-1-butenyl grouping. These D-4-(1'-methyl-3'-oxo-1'-butenyl or alkyl-substituted-1'-methyl-3'-oxo-1'-butenyl)amino-3-isoxazolidinones or 5-methyl derivative thereof, which may also be referred to as N-(1-methyl-3-oxo-1-butenyl or alkyl-substituted-1-methyl-3-oxo-1-butenyl)-derivative of cycloserine or methyl-cycloserine, as well as their pharmacologically acceptable salts, are remarkably stable on storage as well as upon oral administration, and are extremely effective in releasing in vivo the cycloserine compound containing the free primary amino grouping.
REFERENCES:
patent: 2773878 (1956-12-01), Shull et al.
Bassford, Jr. Henry H.
Behan J. Jerome
Merck & Co. , Inc.
Rush Raymond V.
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