Korea Institute of Science and Technology

Youseung Kim

Soon Bang Kang

Seonhee Park

Jae Yang Kong

Dae Young Jeong

Min Seok Jang

Gyochang Keum

Eu Jin Ahn

Taeg-Su Jang

Pyrrolidinone derivatives, their preparation and pharmaceutical composition comprising the same

Tetrahydropyridine derivatives acting on muscarinic acetylcholine receptors

A process for preparing (-)3(S)-methylbenzoxazine derivative of formula (I) comprising the steps of reacting the compound of formula (II) with benzoic acid, triphenylphosphine and diethyl azodicarboxylate in an organic solvent to obtain the compound of formula (III); hydrogenating the compound of formula (III) in the presence of a metallic catalyst to provide the compound of formula (IV); hydrolyzing the compound of formula (IV) to give the compound of formula (V); and reacting the compound of formula (V) with diethyl azodicarboxylate, triphenylphosphine, and zinc chloride in an organic solvent. The obtained (-)3(S)-methylbenzoxazine derivative is a useful intermediate for preparing an antibacterial agent which has a potent bacteriocidal effect. ##STR1##

Process for preparation of (-)3(S)-methylbenzoxazine derivative

There are disclosed (+)2-benzoyl-3-[prop-2(S)-yl)amino] acrylate derivatives of following the formula and a method 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 and R.sub.1 each is an alkyl group containing 1 to 4 carbon atoms.

(+)2-benzoyl-3-[(prop-2(S)-yl)amino]acrylate derivatives and a method

There is disclosed a method for the preparation of the antibacterial (-) piperazine benzoxazine derivative having formula I comprising the steps of reacting (+)2-aminomethylene-3-oxo-3-phenylpropionate derivative of formula II with a base in an organic polar solvent, to give a (-) benzoxazine derivative of formula III: and reacting the (-) benzoxazine derivative of formula III with a piperazine derivative of formula IV in an organic polar solvent. ##STR1##

Method for the preparation of (-)piperazine benzoxazine derivatives

(+)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.

(+) 2-benzoyl-3-(silyloxyprop-2(S)-yl)aminoacrylate derivatives and a

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Seoul, South Korea

Youseung Kim