Abstract: The present invention provides with a process of preparing an optically active succinimide derivative, which is a key intermediate for production of ranirestat. A compound (3) is easily prepared by treating the derivative of succinic acid diester of the formula (2): wherein R1 is an amino group protected with a group removed by hydrogenolysis or a tert-butoxycarbonylamino group and R2 is an ethyl group optionally substituted with one or two methyl group(s) at ?-position, provided that R2 is not a tert-butyl group when R1 is a tert-butoxycarbonylamino group; with alkali metal alkoxide and the compound (3) can be an important intermediate for production of ranirestat.

Abstract: The present invention provides with a process of preparing an optically active succinimide derivative, which is a key intermediate for production of ranirestat. A compound (3) is easily prepared by treating the derivative of succinic acid diester of the formula (2): wherein R1 is an amino group protected with a group removed by hydrogenolysis or a tert-butoxycarbonylamino group and R2 is an ethyl group optionally substituted with one or two methyl group(s) at ?-position, provided that R2 is not a tert-butyl group when R1 is a tert-butoxycarbonylamino group; with alkali metal alkoxide and the compound (3) can be an important intermediate for production of ranirestat.

Abstract: A process for producing a benzoylacrylic acid derivative (formula 1) in high yield through a small number of steps and a simple purification step. The process comprises reacting 2,4,5-trifluoro-3-methyl-6-nitrobenzoyl chloride with a compound (formula 2) to yield an aminoacrylic acid derivative (formula 1) and then reacting the aminoacrylic acid derivative (formula 1) with an amine derivative represented by R2—NH2, wherein R2 is a cycloalkyl group or the like.

Abstract: Novel cephalosporin derivatives of formula (II): ##STR1## wherein R.sup.2 is hydrogen, methyl, or fluoromethyl; R.sup.3 is hydrogen, methyl or carboxyl; R.sup.4 is hydrogen or methyl; A is methylene or propenylene; Q is nitrogen or CH, and pharmaceutically acceptable salts, solvates, hydrates and esters thereof, a process for their preparation and an antimicrobial composition containing them.

Abstract: The present invention relates to a new method for obtaining a purity of about 93% to 100% of the trans form of 2- or 4-substituted cyclohexanecarboxylic acid or reactive derivatives thereof from the cis form or a mixture of the cis and trans forms by a single step, particularly, to a method for obtaining a purity of substantially 100% of the trans form of 4-substituted cyclohexanecarboxylic acid.

Abstract: The invention provides useful intermediates as acylating agents for preparing 7-acylaminocephalosporin compounds which show excellent antimicrobial activities. More particularly, the present invention relates to a process for preparing 5-amino-1,2,4-thiadiazole acetic acid derivatives.

Abstract: An improved process for the production of 5-amino-1,2,4-thiadiazol-3-yl-(2-(lower)-alkoxyimino)acetic acids starting from 5-substituted- or unsubstituted-3-aminoisoxazole compounds is disclosed herein. The title compounds are useful as acylating agents for the production of 7-acylaminocephalosporins.

Abstract: An improved process for the production of 5-amino-1,2,4-thiadiazol-3-yl-(2-(lower)-alkoxyimino)acetic acids starting from 5-substituted- or unsubstituted-3-amino-isoxazole compounds is disclosed herein. The title compounds are useful as acylating agents for the production of 7-acylaminocephalosporins.

Abstract: Herein disclosed are novel cephem compounds represented by the following general formula (I), and novel antimicrobial, and especially anti-MRSA, agents which contain as an active ingredient at least one of the novel cephem compounds and the physiologically acceptable salts thereof.