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Patent Searching and Data


Title:
FLUORO-SUBSTITUTED ADAMANTANE DERIVATIVE
Document Type and Number:
Japanese Patent JPH10298135
Kind Code:
A
Abstract:

To obtain the subject new compound useful as a pharmaceutical composition for curing or preventing a neurological disease, or bacterial or viral infection in a mammal.

A compound of formula I [R1 is NHC(O)R5, etc.; R2 to R4 are each H, fluoro, etc.; R5 is H or a 1-4C alkyl; when R1 is CO2H, R=F and R3 and R4 are not H, and when R1 is NH2, R2=F and R3≠H] or its pharmaceutically permissible salt, e.g. methyl 3-fluoro-5-hydroxyadamantane-1-carboxylate. The compound is obtained, for example, by treating a compound of formula II with diethylaminosulfur trifluoride to obtain the corresponding fluoro substituted ester, hydrolyzing this to convert into an acid of formula III, treating the acid with triethylamine diphenylphosphorylamide and benzyl alcohol, heating the reaction product up to the reflux temperature to obtain a benzylcarbamate intermediate and converting this into an amine of formula IV having a fluoro group on a bridge head carbon of the adamantane.


Inventors:
JASYS VYTAUTUS JOHN
VOLKMANN ROBERT ALFRED
Application Number:
JP9770798A
Publication Date:
November 10, 1998
Filing Date:
April 09, 1998
Export Citation:
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Assignee:
PFIZER
International Classes:
A61K31/00; A61K31/16; A61K31/19; A61K31/215; A61K47/48; A61P25/16; A61P25/28; A61K31/13; A61P31/00; A61P31/04; A61P31/10; A61P31/12; C07C17/16; C07C22/00; C07C51/363; C07C61/15; C07C69/00; C07C69/753; C07C69/757; C07C209/74; C07C211/38; C07C271/24; (IPC1-7): C07C61/15; A61K31/13; A61K31/16; A61K31/19; A61K31/215; C07C69/757; C07C211/38
Attorney, Agent or Firm:
Kazuo Shamoto (4 outside)