(+) 2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivatives and a method for preparing the same
AssigneeKorea Institute of Science and Technology
InventorsYouseung Kim, Soon Bang Kang, Seonhee Park
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Abstract
(+)2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivative of following formula I which can be an useful starting material for producing a potent antibacterial compound and a method for the preparation of the same: ##STR1## wherein X is fluoro or chloro; X.sub.1 and X.sub.2 can be halogen or nitro; and R, R.sub.1, R.sub.2 and R.sub.3 each can be C.sub.1-8 alkyl group.
Claims8
A (+)2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivative having formula I:
- ##STR10## wherein X is fluoro or chloro;
- X.sub.1 and X.sub.2 can be halogen or nitro;
- and R, R.sub.1, R.sub.2, and R.sub.3 each can be C.sub.1-8 alkyl group.
A (+) silyloxyacrylate derivative having formula V:
- ##STR11## wherein R, R.sub.1, R.sub.2, and R.sub.3 each can be C.sub.1-8 alkyl group.
A method for preparing a (+)silyloxyacrylate derivative of formula V which comprises reacting (+) acrylate derivative of formula III with trialkylsilylchloride of formula IV in organic solvent at a temperature of 0.degree. to 30.degree. C. for 1 hour to 24 hours in the presence of a base:
- ##STR12## wherein R, R.sub.1, R.sub.2, and R.sub.3 can be C.sub.1-8 alkyl group.
A method for producing (+)2-benzoyl-3-(silyloxyprop-2(S)-yl) aminoacrylate derivative of the following formula I which comprises reacting (+)silyloxyacrylate derivative of formula (V) with benzoylchloride derivative of formula (VI) in organic solvent at a temperature of 0.degree. to 100.degree. C. for 30 minutes organic solvent at a temperature of 0.degree. to 100.degree. C. for 30 minutes to 12 hours in the presence of a base:
- ##STR13## wherein X is fluoro or chloro;
- X.sub.1 and X.sub.2 can be halogen or nitro;
- R, R.sub.1, R.sub.2, and R.sub.3 each can be C.sub.1-8 alkyl group.
Dependencies are inferred from the claim text.