C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/215, 260/244
C07D 498/04 (2006.01) A61K 31/535 (2006.01) C07D 265/36 (2006.01) C07D 413/06 (2006.01) C07D 498/06 (2006.01)
Patent
CA 1304080
ABSTRACT OF THE DISCLOSURE An optically active pyridobenzoxazine derivative, a process for preparing the same and a novel intermediate useful for preparing the optically active Pyridobenzoxazine derivative are disclosed. The optically active pyridobenzo- xazine derivative of the general formula (VI): Image (VI) wherein X1 represents a halogen atom, R1 represents an alkyl group having 1 to 4 carbon atoms, and R3 represents an alkyl group having 1 to 3 carbon atoms, possess increased antimicrobial activity and reduced toxicity. The intermediate is useful for preparing such optically active pyridobenzoxazine derivatives such as Ofloxacin and anolog compounds. The novel intermediate has the following general formula (X): Image (X) wherein X1 and X2, which may be the same or different, each represents a halogen atom, such as a fluorine atom, a chlorine atom, and preferably both X1 and X2 are fluorine atoms; R1 represents an alkyl groups having from 1 to 4 carbon atoms, such as a methyl group, an ethyl group, a propyl group, etc., and preferably a methyl group; Q repre- sents a hydrogen atom or a group Image wherein R2 represents a substituted sulfonyl group, an alkoxycarbon- yl group or an aralkyloxycarbonyl group, such as a p- toluenesulfonyl group, a benzenesulfonyl group, a methane- sulfonyl group, a t-butoxycarbonyl group, a benzyloxycarbon- yl group, a p-methoxybenzyloxycarbonyl group, etc., prefera- bly a substituted sulfonyl group, and more preferably a p- toluenesulfonyl group; and n represents an integer of from 1 to 3, and preferably 1 or 2.
512000
Atarashi Shohgo
Hayakawa Isao
Higashihashi Nobuyuki
Imamura Masazumi
Ohshima Masayuki
Daiichi Sankyo Company Limited
Riches Mckenzie & Herbert Llp
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