2-benzoyl-3-aminoacrylate derivatives and methods for the prepar

Details 2-benzoyl-3-aminoacrylate derivatives and methods for the prepar 2-benzoyl-3-aminoacrylate derivatives and methods for the prepar

1994-10-11

1996-02-13

Dees, Jose G.

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

Organic compounds

Carboxylic acid esters

560 37, C07C20506, C07C22930

Patent

active

054912512

ABSTRACT:
2-benzoyl-3-aminoacrylate derivatives of the following formula I and methods for the preparation of the same. ##STR1## wherein X is a halogen; X.sub.1 and X.sub.2 are independently selected from a halogen and a nitro; and R, R.sub.1 and R.sub.2 each is an alkyl group containing 1 to 4 carbon atoms. The compounds can be used as starting materials to synthesize benzoxazine derivatives, potent antibacterial compounds.

REFERENCES:
Chemical Abstract 154342 107:704 (1987).
Mitscher, et al., "Chiral DNA Gyrase Inhibitors. 2. Asymmetric Synthesis and Biological Activity of the Enantiomers of 9-Fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[ 1,2,3-de]-1,4-benzoxazine-6-carboxylic Acid (Ofloxacin)", J. Med. Chem., 30:2283 (1987).
Hayakawa, et al., "Synthesis an antibacterial Activities of Substituted 7-Oxo-2,3-dihydro-7H-pyrido-[1,2,3,-de][1,4] benzoxazine-6-carboxylic Acids", Chem. Pharm. Bull., 32:4907-4913 (1984).

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