Process for preparing pyrido-benzothiazine derivatives having hi

Details Process for preparing pyrido-benzothiazine derivatives having hi Process for preparing pyrido-benzothiazine derivatives having hi

1989-12-07

1991-11-19

Lee, Mary C.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D27902

Patent

active

050668021

ABSTRACT:
A process for preparing pyrido-benzothiazine derivatives having the following general formula: ##STR1## in which R is H or a C.sub.1 -C.sub.6 alkyl or a C.sub.1 -C.sub.6 fluoroalkyl, and R.sub.1 is N-alkyl-3-pyrrolidinalkylamine with C.sub.1 to C.sub.6 alkyls or ##STR2## where R.sub.2 is a C.sub.1 -C.sub.6 alkyl or a C.sub.2 -C.sub.6 alkenyl or an arylalkyl group, possibly substituted by halogen, hydroxy or keto-groups, both in the racemic form and in the optically active form. The process for the preparation of derivatives of formula (I) starts with a first reaction cycle starting from 2,4-difluoro-3-chloronitrobenzene. Said derivatives possess a high antibacterial activity as well as a high bioavailability to tissues. The invention also refers to pharmaceutical compositions containing them as active components.

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V. Cecchetti et al., "Quinolonecarboxylic Acids. 2. Synthesis and Antibacterial Evaluation of 7-Oxo-2,3-Dihydro-7H-Pyrido [1,2,3-de][1,4]Benzothiazine-6-Carboxylic Acids", J. Med. Chem. 1987, 30, 465-473.

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