Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

Abstract: It is an object of the present invention to provide a method for synthesizing ?-lactams and a method for manufacturing ?-lactams in water of high-temperature and under high-pressure, and the present invention relates to a ?-lactam synthesis method which is characterized in that ?-lactams are synthesized by reacting ?-amino acids in water at high-temperature and under high-pressure, this method being further characterized in that ?-lactams are synthesized at a high speed by cyclizing ?-amino acids in water at high-temperature and under high-pressure in which the temperature range is 200° C. or higher and the pressure range is 10 MPa or greater, and the present invention also relates to a method for manufacturing ?-lactams which is characterized in that ?-lactams are synthesized by reacting ?-amino acids in water at high-temperature and under high-pressure, and are then separated and purified using a column separation medium.

Abstract: The present discovery consists in new thiazole-substituted ?-lactams of general formula (I), as well as the method for their preparation. R1, R2, R3, R4, R5, R6, R7, and R8 are, independently from each other, a hydrogen atom, a halogen, a hydroxy, amino, nitro, or thiol group, an optionally substituted alkyl, heteroalkyl, aryl, aralkyl, cycloalkyl, cycloaralkyl, heterocycloalkyl, heteroaralkyl, or heteroaryl rest.

Abstract: The present invention relates to a method for the preparation of a compound of the general formula (I) wherein

Abstract: The invention relates to novel 2-bromo- and 2-nitroxy derivatives of 3-,bromo- and 3-dibromo-4-oxo-azetidines, to processes for the preparation thereof and to the use thereof.According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic lanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.

Abstract: Novel 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines, to processes for the preparation thereof and to the use thereof are provided. The azetidines of the present invention have the formula I ##STR1## wherein R.sup.1 is hydrogen or bromine,R.sup.2 is hydrogen or bromine, wherein at least one of R.sup.1 or R.sup.2 is bromine,R.sup.3 is hydrogen; Me.sub.2 --C.dbd.C--COOR.sup.4 wherein R.sup.4 is hydrogen, methyl, benzyl or some other carboxy-protective group, andX is bromine or nitroxy group (--ONO.sub.2).According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.

Abstract: 3-Bromo- and 3,3-dibromo-4-oxo-1-azetidines of the formula I ##STR1## wherein R.sub.1 is hydrogen or bromo,R.sub.2 is hydrogen or bromo,R.sub.3 is hydrogen, ##STR2## wherein R.sub.4 is hydrogen, methyl, benzyl or some other protective group,R.sub.5 is hydrogen, alkyl, alkylaryl, a heterocyclic ring,Y is a halo atom,X is a halo atom, alkoxy group, nitroxy group are provided along with processes for the preparation thereof and the use thereof.

Abstract: This invention provides a process for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, particularly for azetidinones substituted in the C-3 and C-4 positions and optionally substituted at the ring nitrogen, comprising reacting a .beta.-(substituted-amino)amide, a .beta.-(substituted-amino)acid ester, or a .beta.-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent.

Abstract: The azetidines of the present invention have the formula I ##STR1## wherein R.sup.1 is hydrogen or bromine,R.sup.2 is hydrogen or bromine, wherein at least one of R.sup.1 or R.sup.2 is bromine,R.sup.3 is hydrogen; Me.sub.2 --C.dbd.C--COOR.sup.4 wherein R.sup.4 is hydrogen, methyl, benzyl or some other carboxy-protective group, andX is bromine or nitroxy group (--ONO.sub.2).According to the invention 2-bromo- and 2-nitroxy derivatives of 3-bromo- and 3-dibromo-4-oxo-azetidines are prepared by reacting derivatives of protected penicillanic acid 1,1-dioxides with DBN reactant (1,5-diazabicyclo/3.4.

Abstract: A process for preparing compounds of the formula ##STR1## wherein R and R.sup.2 are independently --OH, --O(lower alkyl) or --0-benzyl and the remaining variables are as defined in the specification, comprising(a) treating with a strong base in an anhydrous organic solvent a lactone of the formula ##STR2## respectively, wherein Ar.sup.10 is Ar.sup.1 or a suitably protected hydroxy- or amino-substituted aryl, and R' and R.sup.2' are R and R.sup.2 as defined above or are suitably protected hydroxy groups;(b) reacting a product of step (a) with an imine of the formula ##STR3## wherein Ar.sup.20 and Ar.sup.30 are Ar.sup.2 or Ar.sup.3 or suitably protected hydroxy- or amino-substituted aryl;c) quenching the reaction with an acid; andd) removing protecting groups as necssary.

Abstract: Azetidinones of the formula I ##STR1## in which, for example, R.sup.1 is an alkyl or alkenyl radical, R.sup.2 and R.sup.3 are hydrogen or an alkyl or alkenyl radical, Z is hydrogen or (pseudo)halogen, A.sup.1, A.sup.2 and A.sup.3 are a ring system, and M is a spacer group, can be added to liquid-crystal mixtures. Even when admixed in small amounts, they cause considerable twist in the cholesteric and smectic C* phase, which can compensate the pitch of another dope or produce a short S.sub.C * pitch.

Abstract: Compounds of the structural formulae ##STR1## and their pharmaceutically acceptable salts, esters and amide derivatives, in which R.sup.1 and R.sup.2, independently of one another, denote hydrogen or pharmaceutically acceptable groups which have 1 to 10 carbon atoms and are bonded to the remaining part of the molecule via carbon-carbon single bonds, and in which R.sup.3, R.sup.4 and R.sup.5, independently of one another, denote pharmaceutically acceptable groups which have 1 to 10 carbon atoms and are bonded to the remaining part of the molecule via carbon-carbon single bonds, are useful antibiotics.The trisubstitution by three groups R.sup.3, R.sup.4 and R.sup.5, which are bonded via carbon-carbon single bonds, results in a noticeable increase in the hydrolysis stability and thus also in the antibacterial action of axapenemcarboxylic acids.

Abstract: This invention provides novel azetidinone intermediates having the formulas: ##STR1## wherein R.sup.1 is hydrogen, or a conventional hydroxy-protecting groups; R.sup.2, R.sup.4, and R.sup.5 are independently selected from the group consisting of hydrogen; substituted and unsubstituted: alkyl, alkenyl, and alkynyl having from 1-10 carbon atoms; cycloalkyl, cycloalkylalkyl, and alkylcycloalkyl having 3-6 carbon atoms in the cycloalkyl ring and 1-6 carbon atoms in the alkyl moieties; spirocycloalkyl having 3-6 carbon atoms; phenyl; aralkyl, aralkenyl, and aralkynyl wherein the aryl moiety is phenyl and the aliphatic portion has 1-6 carbon atoms; or various heterocyclic moieties; and R.sup.6 is methanesulfonyl or p-toluenesulfonyl; which are useful in the preparation of carbapenem antibiotics.

Abstract: An intermediate for synthesizing carbapenems is produced through(1) a reaction of 4-(leaving group substituted)-2-azetidinone (I) with (alk-2-enyl)halosilane (II) to afford 4-(leaving group substituted)-1-(alk-2-enyl)silyl-2-azetidinone (III) and then(2) a reaction of the product 4-(leaving group substituted)-1-alk-2-enyl)silyl-2-azetidinone (III) with acid to give the corresponding 4-(alk-2-enyl)-2-azetidinone (IV).

Abstract: The invention relates to new 2-oxoazetidines having the formulas ##STR1## where R.sub.1 stands for a lower fluoroalkyl or an optionally protected lower hydroxyalkyl group; R.sub.2 for chlorine, bromine, iodine, fluorine, an ##STR2## group in which n is 0, 1 or 2 and R.sub.5 is a lower alkyl, lower alkenyl, an optionally substituted benzyl group, optionally substituted phenyl group, a --CH.sub.2 COX group in which X means a lower alkyl, lower alkoxy or the amino group, or a ##STR3## group in which Y and Z are the same or different and in each case stand for oxygen, nitrogen or sulphur and R.sub.6 stands for a lower alkyl, lower alkoxy, lower alkylthio, lower dialkylamino, an aryl, aryloxy or arylthio group, or for a group having the formula ##STR4## where W stands for --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or C.sub.6 H.sub.4 ; R.sub.3 stands for bromine, chlorine, iodine, SeC.sub.6 H.sub.5 or SC.sub.6 H.sub.5 ; and R.sub.4 stands for hydrogen, a group having the formula ##STR5## in which R.sub.

Abstract: There is disclosed a process for producing carbapenam diazo intermediates of the formula ##STR1## wherein R.sup.1 is hydrogen or a hydroxy-protecting group,R.sup.2 is a lower alkyl having from 1-6 carbon atoms, andR.sup.3 represents a conventional carboxyl-protecting group.The processs comprises alkylating a 4-substituted azetidinone with the tin enolate of an .alpha.-bromoketone, in the presence of a silver salt, iodine, or iodine salt as a catalyst, and a strongly polar solvent. The .beta./.alpha. yield of the product diazo intermediate is approximately 3/1.

Abstract: New substituted azetidinones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: Certain substituted-2-penem-3-carboxylic acid compounds, and pharmaceutically-acceptable salts thereof, can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization, followed by halogenation and ring closure. The corresponding desulfurized and halogenated intermediates are disclosed.