Abstract: There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1.beta.-methylcarbapenem-type antibacterial agent.

Abstract: There is disclosed an azetidinone compound of the formula ?I!: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1 .beta.-methylcarbapenem-type antibacterial agent.

Abstract: Novel process for preparing azetidinone compound of the formula ?III!: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula ?I!: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula ?II!: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound ?Ill! being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.

Abstract: Novel butadiene derivatives of the formula [I]: ##STR1## wherein Ring A is tri-lower alkoxyphenyl, R.sup.1 and R.sup.2 combine each other to form a group of the formula: ##STR2## or one of R.sup.1 and R.sup.2 is lower alkoxy, and the other is group of the formula: -NHR.sup.3, in which R.sup.3 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof, these compounds have excellent antithrombotic activity and are useful as antithrombotic drug, or synthetic intermediate for preparing other antithrombotic drug.

Abstract: There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1.beta.-methylcarbapenem-type antibacterial agent.

Abstract: A method for removing substituted or unsubstituted allyl group from .beta.-lactam compound having substituted or unsubstituted allyl group-protecting carboxyl group, which comprises treating said .beta.-lactam compound with palladium catalyst in the presence of allyl-scavenger in aqueous organic solvent, by which the substituted or unsubstituted group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.

Abstract: Novel process for preparing azetidinone compound of the formula [III]: ##STR1## wherein R.sup.1 is H or lower alkyl, R.sup.2 and R.sup.3 combine together with the adjacent nitrogen to form heterocyclic group, and R.sup.4 is protected or unprotected hydroxy-substituted lower alkyl, which comprises reacting an alkanamide compound of the formula [I]: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are the same as defined above, with a compound of the formula [II]: ##STR3## wherein L.sup.1 is a leaving group and R.sup.4 is the same as defined above, in the presence of a base, said compound [III] being useful as synthetic intermediate for 1-methylcarbapenem derivative having excellent antibacterial activity.

Abstract: Novel succinimide derivatives of formula I!: ##STR1## wherein Ring A is tri-lower alkoxyphenyl, R.sup.1 and R.sup.2 combine each other to form a group of the formula:>N--R.sup.3or one of R.sup.1 and R.sup.2 is lower alkoxy, and the other is group of the formula: --NHR.sup.3, in which R.sup.3 is hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted amino, hydroxy or pyridylcarbonyl, or salts thereof, these compounds have excellent antithrombotic activity and are useful as antithrombotic drug, or synthetic intermediate for preparing other antithrombotic drug.

Abstract: A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula [I]: ##STR1## wherein R.sup.1 is a hydrogen atom or a protecting group and R.sup.2 is a hydrogen atom or a protecting group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.

Abstract: There is disclosed an azetidinone compound of the formula [I]: ##STR1## wherein Ring B is a benzene ring which may have substituent(s), R.sup.1 is a hydroxy-substituted lower alkyl group which may have substituent(s), X is oxygen atom and the like, Y is oxygen atom and the like, and Z is a methylene group which may have substituent(s), which is useful as a synthetic intermediate of the 1.beta.-methylcarbapenem-type antibacterial agent.

Abstract: A process for preparing an optically active 4-mercapto-2-pyrrolidone derivative of the formula: ##STR1## wherein a group of the formula: --SR.sup.1 is a protected or unprotected mercapto group, and the group of the formula: .dbd.NR.sup.2 is a protected or unprotected imino group, which comprises subjecting racemic 4-amino-3-mercaptobutyric acid or a salt thereof to optical resolution by using 1-(2,3,4-trichlorophenyl)ethanesulfonic acid, followed by subjecting the product to cyclization reaction after protecting the functional groups thereof, if necessary, and further optionally removing the protecting groups therefrom. The present process is industrially advantageous than conventional processes for preparing optically active 4-mercapto-2-pyrrolidone derivatives which are useful as an intermediate for various medicines such as carbapenem antibacterial agents.

Abstract: Disclosed is a process for preparing a .beta.-lactam compound represented by the formula: ##STR1## wherein R.sup.1 represents a hydroxy-substituted lower alkyl group or an amino group each of which may be protected; R.sup.2 represents hydrogen atom or an ester residue; X represents a methylene group which may be substituted by a lower alkyl group, sulfur atom or a group represented by the formula: --A--CH.sub.2 -- where A represents sulfur atom, oxygen atom or methylene group; and W represents an active ester residue of hydroxyl group, or a salt thereof, which comprises the steps of treating a 1-aza-3-thia-bicycloalkane compound represented by the formula: ##STR2## wherein R.sup.1, R.sup.2 and X have the same meanings as defined above, or a salt thereof with a base in the presence of a desulfurizing agent and then reacting the resulting compound with an active esterifying agent of hydroxyl group.

Abstract: Process for preparing carbapenem derivative of the formula [I], which comprises subjecting azetidinone compound of the formula [II] to intramolecular cyclization reaction together with elimination reaction of the group of --SR.sup.4, followed by re-adding said group of --SR.sup.4 to the 2-position of the carbapenem skeleton of the intramolecularly cyclized compound, which is industrially useful as process for preparing carbapenem antimicrobials or synthetic intermediate therefor. ##STR1## wherein R.sup.1 is protected or unprotected hydroxy-substituted lower alkyl group, R.sup.2 is hydrogen atom or ester residue, R.sup.3 is hydrogen atom or lower alkyl group, and the group of --SR.sup.4 is group which can be used as substituent at 2-position of the carbapenem antimicrobials.

Abstract: Naphthalene derivative of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen atom, hydroxy group, cyclo-lower alkyloxy group, substituted or unsubstituted lower alkoxy group, or both combine each other to form lower alkylenedioxy group, R.sup.3 is substituted or unsubstituted nitrogen-containing 6-membered heterocyclic group, and groups of the formulae: --OR.sup.4 and --OR.sup.5 are the same or different and are protected or unprotected hydroxy group, processes for preparing thereof, and synthetic intermediates therefor, these compounds have excellent bronchodilating activity, and are useful in the prophylaxis and treatment of asthma.

Abstract: Disclosed are a dicarboxylic acid compound represented by the formula (I): ##STR1## wherein R represents hydrogen atom, a lower alkyl group, phenyl group or hydroxyl group; R.sup.1 represents a straight or branched alkyl group having 1 to 10 carbon atoms or a lower alkyl group substituted by a group selected from aryl group, a sulfur- or nitrogen-containing heterocyclic monocyclic group and a cycloalkyl group having 4 to 8 carbon atoms; R.sup.2 represents a substituted or unsubstituted aryl group, a cycloalkyl group having 4 to 8 carbon atoms or a sulfur-containing or nitrogen-containing heterocylcic group; X represents sulfur atom, oxygen atom or a substituted or unsubstituted imino group; Y.sup.1 represents imino group, oxygen atom or sulfur atom and Y.sup.2 represents nitrogen atom, or Y.sup.1 represents a vinylene group and Y.sup.2 represents a group: --CH.dbd.

Abstract: A method for removing tri-substituted silyl group from .beta.-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.

Abstract: Novel biphenyl derivatives of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted aminocarbonyl group, aminothiocarbonyl group, a substituted or unsubstituted lower alkoxycarbonyl group, cyano group, or a group of the formula: ##STR2## one or two of R.sup.2 to R.sup.7 are hydrogen atom, and the remaining groups are the same or different and are each a lower alkoxy group, a phenyl(lower)alkoxy group or hydroxy group, or the adjacent two groups thereof combine to form a lower alkylenedioxy group, and Alk.sup.1 is a lower alkylene group, or a pharmaceutically acceptable salt thereof, which are useful for the prophylaxis and treatment of hepatic diseases, and processes for preparing the same, and intermediates therefor.

Abstract: A mercaptan compound of the formula ##STR1## wherein R.sup.3 is a hydrogen atom or a lower alkyl group, or a salt thereof.

Abstract: Novel biphenyl derivatives of the formula: ##STR1## wherein R.sup.1 is a substituted or unsubstituted aminocarbonyl group, aminothiocarbonyl group, a substituted or unsubstituted lower alkoxycarbonyl group, cyano group, or a group of the formula: ##STR2## one or two of R.sup.2 to R.sup.7 are hydrogen atom, and the remaining groups are the same or different and are each a lower alkoxy group, a phenyl-(lower)alkoxy group or hydroxy group, or the adjacent two groups thereof combine to form a lower alkylenedioxy group, and Alk.sup.1 is a lower alkylene group,or a pharmaceutically acceptable salt thereof, which are useful for the prophylaxis and treatment of hepatic diseases, and processes for preparing the same, and intermediates therefor.

Abstract: A novel biphenyl derivative of the formula: ##STR1## wherein Ring A is a substituted or unsubstituted sulfur-containing or oxygen-containing heteromonocyclic ring; Ring B is a ring of the formula: ##STR2## each of R.sup.1 to R.sup.3 is hydrogen atom, a halogen atom or a lower alkoxy group, or R.sup.1 is hydrogen atom, and R.sup.2 and R.sup.3 are combined together to form a lower alkylenedioxy group; R.sup.4 is a lower alkyl group which may have a substituent selected from a lower alkoxy group and a lower alkoxycarbonyl group; Y is methylene group or carbonyl group, and a pharmaceutically acceptable salt thereof are disclosed. Said derivative and a pharmaceutically acceptable salt thereof are useful as a therapeutic or prophylactic agent for hepatic diseases.