摘要:
Disclosed are 2.beta.-substituted-methylpenicillanic acid compounds of the formula ##STR1## wherein n is 0, 1 or 2; and ##STR2## is monocyclic or bicyclic heterocyclic ring group which has 2 to 4 nitrogen atoms as hetero atom in its ring structure and which may be optionally substituted with alkyl, alkoxycarbonyl, phenyl, formyl or benzyloxycarbonyl optionally having alkyl, nitro or a halogen atom on the benzene ring, with the proviso that said heterocyclic ring group is not 1,2,3-triazol-1-yl; or salts or esters thereof.These compounds are useful as .beta.-lactamase inhibitor.
摘要:
Disclosed is a process for preparing 2.beta.-substituted-methylpenicillin derivative of the formula ##STR1## wherein R is H or carboxyl protecting group, R.sub.1 is H or halo, R.sub.2 is H, lower alkyl, lower alkoxy, halogen, azido, lower alkylthio, phthalimide or a group --NHR.sub.3 (wherein R.sub.3 is H or acyl), and --N Y is an optionally substituted monocyclic or bicyclic heterocyclic group having 1 to 4 nitrogen atoms in the ring structure, the process comprising reacting a compound of the formula ##STR2## wherein X is Cl or Br, and R, R.sub.1 and R.sub.2 are as defined above with a heterocyclic compound of the formula ##STR3## wherein --N Y is as defined above.
摘要:
Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.
摘要:
2.alpha.-Methyl-2.beta.-(1,2,3-triazol-1-yl)methylpenam-3.alpha.-carboxylic acid derivatives are prepared by reacting a penicillanic acid sulfoxide derivative of the formula ##STR1## wherein R is a penicillin carboxyl protecting group, and R.sub.1 is hydrogen or halogen, R.sub.2 is hydrogen, lower alkyl or the like with a triazole derivative of the formula ##STR2## wherein R.sub.3 and R.sub.4 are hydrogen, trialkylsilyl, lower alkyl, lower alkoxy or the like and R.sub.5 is hydrogen or silyl substituted with 3 groups selected from the class consisting of lower alkyl, benzyl and phenyl in a solvent.
摘要:
A process for preparing a 2.beta.-substituted-methylpenicillin compound of the formula ##STR1## wherein --N Y is an optionally substituted heterocyclic group containing 2 to 4 nitrogen atoms as the hetero atom in the ring structure, and R.sub.1 is a penicillin carboxyl protecting group, the process comprising reacting an azetidinonedisulfide compound of the formula ##STR2## wherein R.sub.1 is as defined above and R is a substituted or unsubstituted heterocyclic group with a nitrogen-containing heterocyclic compound of the formula ##STR3## wherein ##STR4## is as defined above in the presence of a metal compound.
摘要:
The present invention provides a process for preparing a penicillanic acid derivative of the formula ##STR1## which comprises reacting lead with a halogenated penicillanic acid derivative of the formula ##STR2## wherein X, Y, Z and R.sup.1 are as defined in the specification. The reaction is advantageously conducted in the presence of a metal having higher ionization tendency than lead such as aluminum, iron, magnesium or a mixture thereof.
摘要:
This invention is to provide a process for preparing 1-amino-1,2,3-triazole represented by formula (III): ##STR1## comprising cyclizing glyoxal bishydrazone represented by formula (I): ##STR2## by reaction with an aqueous hydrogen peroxide solution in the presence of a catalytic amount of a transition metal oxide represented by formula (II): M.sub.m O.sub.n wherein M represents a transition metal atom; and m and n, which may be the same or different, each represent an integer of 1 to 5.
摘要:
A mixture of an isomer of 2,2'-azobis(2,4-dimethylvaleronitrile) having a low melting point in an amount of about 70% by weight or more and an isomer of 2,2'-azobis(2,4-dimethylvaleronitrile) having a high melting point in an amount of about 30% by weight or less shows excellent solvent solubility, which is higher than that of the isomer having a low melting point. The mixture is useful as a polymerization initiator, and also as a blowing agent.
摘要:
An improved process for preparing oxytitanium phthalocyanine is provided wherein the condensation reaction of o-phthalodinitrile with titanium tetrachloride is effected in an organic solvent at 170.degree. to 300.degree. C. followed by hydrolysis, the improvement wherein said organic solvent is preliminarily heated at a temperature of 160.degree. to 300.degree. C. prior to initiation of the condensation reaction. The A form of oxytitanium phthalocyanine crystal can selectively be produced in the pure state.
摘要:
A silver halide photosensitive material comprising a support, a silver halide photosensitive layer, and a protective layer formed on said support. The protective layer is essentially composed on a plurality of non-photosensitive hydrophilic colloidal layers at least one of which contains oil particles. The outermost layer of the hydrophilic colloidal layers contains a matting agent in the form of colloidal particles and has a thickness of not more than one fourth of the average size of the matting agent particles and wherein the density of the oil particles in said outermost layer does not exceed 0.2 by volume of the binder, and that of the oil particles in the protective layers other than the outermost layer is in the range of 0.1 to 0.8.