PRODUCTION OF 4-DEDIMETHYLAMINO-12A-DEOXYTETRACYCLINE

PURPOSE:To obtain 4-dedimethylamino-12a-deoxytetracycline useful for nodose rheumatism, periodontal diseases, etc., by hydrolyzing a specific 4- dedimethylaminotetracyclin-12a-ester derivative in a solvent in the presence of a metal catalyst. CONSTITUTION:A 4-dedimethylaminotetracyclin-12a-ester der...

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Bibliographic Details
Main Authors HAMAZAKI TAKASHI, KIKUYAMA SHIGEKI, KAWAI TSUTOMU, TAKIGAWA TETSUO
Format Patent
LanguageEnglish
Published 18.01.1994
Edition5
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Summary:PURPOSE:To obtain 4-dedimethylamino-12a-deoxytetracycline useful for nodose rheumatism, periodontal diseases, etc., by hydrolyzing a specific 4- dedimethylaminotetracyclin-12a-ester derivative in a solvent in the presence of a metal catalyst. CONSTITUTION:A 4-dedimethylaminotetracyclin-12a-ester derivative of formula I (R is H, alkyl, aryl or aralkyl) (e.g. 4-dedimethylamino-12a-formyltetracycline) is hydrolyzed in a solvent such as tetrahydrofuran in the presence of a metal catalyst (preferably palladium carbon or Raney nickel) to give 4- dedimethylamino-12a-deoxytetracycline of formula II and formula III. 4- Dedimethylamino-12a-deoxytetracycline is useful for treating diseases characterized by excessive destruction of collagen such as nodose rheumatism, periodontal diseases, etc.
Bibliography:Application Number: JP19920185902