Abstract: To provide a compound which exhibits excellent anti-tumor activity and excellent oral absorption and which is a useful anti-tumor drug. The invention provides a 3?-ethynylcytidine derivative represented by formula (1): (wherein X represents a (substituted) alkylcarbonyl group, a (substituted) alkoxycarbonyl group, or a hydrogen atom; one of Y and Z represents a hydrogen atom or a group represented by (R1)(R2)(R3)Si— and the other represents a group represented by (R4)(R5)(R6)Si—; and R1, R2, R3, R4, R5, and R6 each represent a (substituted) alkyl group, a (substituted) cyclic alkyl group, or a (substituted) aryl group) or a salt thereof.

Abstract: To provide a compound which exhibits excellent anti-tumor activity and excellent oral absorption and which is a useful anti-tumor drug. The invention provides a 3?-ethynylcytidine derivative represented by formula (1): (wherein X represents a (substituted) alkylcarbonyl group, a (substituted) alkoxycarbonyl group, or a hydrogen atom; one of Y and Z represents a hydrogen atom or a group represented by (R1)(R2)(R3)Si— and the other represents a group represented by (R4)(R5)(R6)Si—; and R1, R2, R3, R4, R5, and R6 each represent a (substituted) alkyl group, a (substituted) cyclic alkyl group, or a (substituted) aryl group) or a salt thereof.

Abstract: The present invention relates to D-pentofuranose derivatives represented by the following formulas (1) through (4): ##STR1## (wherein A represents a chlorobenzoyl group; R.sup.1 represents a hydrogen atom, an aliphatic lower acyl group, a substituted or unsubstituted benzoyl group; each of X and Y represents a lower alkyl group; Z represents an ethynyl group or tri-lower alkyl silylethynyl group; the sugar moiety in formula (1) represents xylose; and the sugar moiety of each of formulas (3) and (4) represents ribose). The present invention also relates to a process for preparing the compound (2) characterized by oxidizing the compound of formula (1) with a hypochlorite in the presence of a catalytic amount of 2,2,6,6-tetramethylpiperidinoxy compound, and these compounds are useful as intermediates in the synthesis of 3'-C-substituted ribonucleoside derivatives having excellent antitumor activities.

Abstract: 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.nwherein 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.

Abstract: The present invention provides a process for producing isoxazole derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each a hydrogen atom or lower alkoxyl, and R.sup.3 is cyano or alkoxycarbonyl, the process being characterized by oxidizing an .alpha., .beta.-unsaturated ketoxime derivative represented by the formula ##STR2## wherein R.sup.1 , R.sup.2 and R.sup.3 are as defined above. The isoxazole derivatives (II) to be produced by the process of the present invention are useful as intermediates for preparing (3,4-diarylisoxazol-5-yl) acetic acid derivatives which are useful as anti-inflammatory agents, analgesics and antipyretics.

Abstract: The present invention provides an .alpha., .beta.-unsaturated ketone and ketoxime derivative represented by the formula ##STR1## wherein Y is oxygen atom or hydroxyimino group, Z is cyano or alkoxycarbonyl group, R.sup.1 and R.sup.2 are the same or different and are each hydrogen atom or lower alkoxyl group.The .alpha., .beta.-unsaturated ketones and ketoxime derivatives of the invention are useful as an intermediate for preparing a (3,4-diarylisoxazol-5-yl)acetic acid derivatives which is useful as an anti-inflammatory agent, analgesic and antipyretic.

Abstract: Cyclic azoamidine compounds having the formula and salts thereof are disclosed. ##STR1## wherein R denotes a methyl group or an ethyl group, and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently denote a lower alkyl group having one to four carbon atoms or a hydrogen atoms, provided that a case where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are all hydrogen atoms is excluded. The cyclic azoamidine compounds and their salts are useful as polymerization initiators in the production of polymer compounds.

Abstract: An azoimino ether, which is an intermediate for preparing polymerization initiators, is prepared by reacting a hydrazonitrile having a hydrazo group and at least one cyano group in the molecule with chlorine in the presence of an alcohol, in a non-aqueous organic solvent.

Abstract: 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.

Abstract: Granules of azobisamidine salt can be produced by granulating a powder of azobisamidine salt using a limited amount of water or a mixture of water and a water-soluble organic solvent such as methanol are convenient in handling without deteriorating the quality and can be used as a water-soluble polymerization initiator.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: A process for the preparation of a light-sensitive silver halide photographic material comprising a support, a silver halide emulsion layer, and a non-light-sensitive hydrophilic colloid layer which consists essentially of a plurality of layer elements; a process comprises incorporating oil particles into at least one of the elements, so that the oil particle density of the outermost layer element is not the highest of the oil particle densities of all of the elements.

Abstract: 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.

Abstract: 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.

Abstract: The invention provides an improvement in the suspension polymerization of vinyl chloride in an aqueous medium in the presence of a monomer-soluble polymerization initiator, according to which the amount of polymer scale deposition on the reactor walls can be greatly decreased. The improvement comprises admixing the aqueous polymerization medium with (a) a water-soluble crosslinked copolymer of an unsaturated carboxylic acid monomer, e.g. acrylic acid, and a crosslinking monomer such as di(methyl)allyl ether of diethyleneglycol and (b) a non-ionic surface active agent in combination.

Abstract: The invention provides an improvement in the suspension polymerization of vinyl chloride in an aqueous medium in the presence of a monomer-soluble polymerization initiator, according to which the amount of polymer scale deposition on the reactor walls can be greatly decreased. The improvement comprises admixing the aqueous polymerization medium with (a) a water-soluble crosslinked copolymer of an unsaturated carboxylic acid monomer, e.g. acrylic acid, and a crosslinking monomer such as di(methyl)allyl ether of diethyleneglycol and (b) a non-ionic surface active agent in combination.