Abstract: Provided herein is a taxane having a hydrocarbon attached at the 2' and/or 7 positions, the hydrocarbon's alpha position being occupied by a "hydrolysis-promoting group" ("HPG"). In one embodiment, the hydrolysis promoting group is stereospecifically attached to the .alpha.-carbon of the hydrophobic taxane. The Substitution of an HPG for the methylene unit ordinarily occupying the alpha position allows for enhanced in vivo hydrolysis of the hydrocarbon-taxane bond, and hence, for enhanced taxane therapeutic activity. Also provided herein are taxane-containing compositions, and methods of administering taxanes to animals, including those afflicted with cancers or inflammatory diseases.

Abstract: The compounds 18.beta., 19.beta.-diacetyloxy-18.alpha., 19.alpha.-epoxy-3, 13(16), 14-clerodatrien-2-one (Esculentin A) and 18.beta., 19.beta.-diacetyloxy-18.alpha., 19.alpha.-epoxy-3, 12, 14-clerodatrien-2.beta.-isovaleryloxy-6.beta., 7.alpha.-diol (Esculentin B) obtained from plants belonging to the Samydaceae family, particularly Casearia esculenta, a process for their preparation, and their use in the manufacture of medicaments. The compounds are particularly useful as anti-inflammatory and/or anti-cancer agents.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: C7, C10 di-CBZ 10-deacetyl baccatin III of the formula: ##STR1## provides an intermediate for the production of docetaxel. A method of producing this C7, C10 di-CBZ 10-deacetyl Baccatin III is provided. Here, 10-deacetyl Baccatin III is acylated with at least 1.5 equivalents of n-butyl lithium and at least 1.5 equivalents of benzyl chloroformate in tetrahydrofuran. The 10-deacetyl Baccatin III may first be dissolved in tetrahydrofuran after which the n-butyl lithium is added followed by the addition of the benzyl chloroformate. The reaction is preferably at a reduced temperature of less than -20.degree. C. The resulting solution may be quenched with ammonium chloride and reduced to residue. The residue may then be redissolved in an organic solvent, washed, dried and recrystallized to purify the compound.

Abstract: Process for the production of epoxides by the reaction of at least one olefin and hydrogen peroxide, or a compound capable of producing hydrogen peroxide under the reaction conditions, in the presence of a catalyst consisting of titanium silicalite subjected to ion exchange treatment with metal cations (M.sup.n+) present on the catalyst in a quantity ranging from 0.01 to 1% by weight with respect to the total weight.

Abstract: A novel class of bridged indicator dyes is disclosed which possess absorption in the infrared region of the electromagnetic spectrum. These bridged indicator dyes are useful as light-absorbing, pH-sensitive optical filter agents in diffusion transfer photographic processes adapted to be performed in the presence of ambient light and to diffusion transfer products useful in such processes. These indicator dyes will also find utility in titrations and other analytical techniques and products where pH-sensitive indicator dyes are employed and absorption of infrared is useful.

Abstract: A silver catalyst excelling in catalytic performance and permitting production of ethylene oxide with a high selectivity for a long time, a method for the production of ethylene oxide by the use of the silver catalyst, and a method for ideal manufacture of the silver catalyst are disclosed. The silver catalyst is formed by depositing silver on a carrier having .alpha.-alumina as a main component and used for the production of ethylene oxide, which carrier of the silver catalyst has undergone the following treatment capable of yielding a wash exhibiting a resistivity index of not less than 10,000 .OMEGA..multidot.cm (25.degree. C.):(Method of treatment)In a conical beaker having an inner volume of 500 ml, 300 ml of the carrier is placed, dried therein at 120.degree. C. for two hours, and boiled in conjunction with (water absorption +220) ml of pure water added thereto under normal pressure at 90.degree. C.

Abstract: This invention relates to a taxoid of the formula (I): ##STR1## wherein R.sup.1 is a C.sub.3 -C.sub.5 alkyl or alkenyl or trifluoromethyl radical;R.sup.2 is a C.sub.3 -C.sub.5 branched alkyl radical;R.sup.3 and R.sup.4 are independently selected from hydrogen and hydroxyl protecting groups including functional groups which increase the water solubility of the taxoid antitumor agent;R.sup.5 is a hydrogen, an acyl radical, or an alkoxylcarbonyl or carbamoyl radical; andR.sup.6 is an acyl radical.The compounds of formula I are useful as antitumor agents or their precursors. This invention also relates to a pharmaceutical composition having antineoplastic activity comprising the compound of formula (I) and a physiologically acceptable carrier and method of treatment using the compound of formula I.

Abstract: A process for the production of at least one C.sub.4 compound selected from butane-1,4-diol, .gamma.-butyrolactone and tetrahydrofuran comprises contacting a vaporous stream containing maleic anhydride vapour, water vapour, and carbon oxides in an absorption zone with a high boiling organic solvent thereby to form a solution of maleic anhydride in the high boiling organic solvent. Maleic anhydride in this solution is reacted under esterification conditions in an esterification zone with a C.sub.1 to C.sub.4 alkanol to form a solution of the corresponding di-(C.sub.1 to C.sub.4 alkyl) maleate in the high boiling solvent. This solution of the di-(C.sub.1 to C.sub.4 alkyl) maleate in the high boiling solvent is contacted with a gaseous stream containing hydrogen thereby to strip di-(C.sub.1 to C.sub.4 alkyl) maleate therefrom and to form a vaporous stream comprising hydrogen and di-(C.sub.1 to C.sub.4 alkyl) maleate.

Abstract: A process for producing propylene oxide by reacting propylene with ethylbenzene hydroperoxide in the presence of a titanium-containing silicon oxide catalyst satisfying all of the following conditions (1) to (4):(1): an average pore size of 10 .ANG. or more,(2): a pore size of 90% or more of the total pore volume of 5 to 200 .ANG.,(3): a specific pore volume of 0.2 cm.sup.3 /g or more, and(4): a quarternary ammonium ion represented by the following general formula (I) is used as a template and then said template is removed by solvent extraction operation;[NR.sup.1 R.sup.2 R.sup.3 R.sup.4 ].sup.+ (I)wherein, R.sup.1 represents a linear or branched hydrocarbon chain having 2 to 36 carbon atoms, and R.sup.2 to R.sup.4 represent an alkyl group having 1 to 6 carbon atoms.

Abstract: Polymerizable and hydrolysable oxetane silanes and in particular silicic acid condensates which can be prepared therefrom are described, which exhibit only a low volume shrinkage on polymerization and produce polymers with high mechanical strength and therefore can be used above all as dental material or constituent thereof.

Abstract: This invention relates to a taxoid of the formula (I) ##STR1## wherein R.sup.1 is 1-propenyl radical;R.sup.2 is a C.sub.3 -C.sub.5 branched alkyl radical;R.sup.3 and R.sup.4 are independently selected from hydrogen and hydroxyl protecting groups including functional groups which increase the water solubility of the taxoid antitumor agent;R.sup.5 represents a hydrogen or a hydroxyl protecting group;R.sup.6 represents an acyl radical,which are useful as antitumor agents or their precursors. A pharmaceutical composition having antineoplastic activity comprising the compound of formula (I) and a physiologically acceptable carrier and method of treatment are also disclosed.

Abstract: Epoxides are prepared from olefins using bis(triorganosilyl) peroxides in the presence of activators based on metalic acid derivatives of the formula ##STR1## where M is a metal of transition groups IV to VII, in particular molybdenum, tungsten or rheniumL is an uncharged ligand selected from the group consisting of amine oxides, phosphine oxides, arsine oxides, phosphoric triamides, formamides and pyridine N-oxidesX is an inorganic ligandx is from 1 to 5y is 0, 1 or 2,Z is 1 or 2 andn is 1 or 2.

Abstract: The invention discloses a process for the preparation of a compound, having molecular formula C.sub.29 H.sub.50 O.sub.6 and isomeric structural formulae (2R, 3S, 22R, 23R) -2, 3, 22, 23 -tetrahydroxy-24- ethyl-.beta.-homo-7-oxa -5.alpha.- cholestan-6- one and (2R, 3S, 22S, 23S) -2, 3, 22-23-tetrahydroxy-24- ethyl-.beta.-homo-7-oxa-5.alpha.-cholestan -6- one in a ratio 69:31, both of which are members of a new class of steroidal phytohormones.

Abstract: A process for preparation of a glycidyl ether which is characrelized in reacting an epoxy compound of the formula ##STR1## wherein X is halogen or sulfonyloxy in the presence of a fluoride salt, with an alcohol. According to the above method, glycigyl ethers or their optically active compounds important as intermediates for synthesis of medicines are easily obtained in good yield and especially the optically active compounds are obtained with highly optical purity.

Abstract: The invention provides various derivatives of arglabin, a sesquiterpene lactone isolated from Artemisia glabella. These compounds are effective for suppressing tumor growth in mammals. A method of suppressing tumor growth in humans is also described.

Abstract: The invention provides taxanes that are conjugates of cis-docosahexaenoic acid and taxotere. The conjugates are useful in treating cancer.

Abstract: A novel phosphine compound usable as a catalyst in various asymmetric synthetic reactions is disclosed. The compound is a 2,2'-bis(diarylphosphino)-6,6'-bis(trifluoromethyl)-1,1'-biphenyl of (1): ##STR1## where R is a phenyl group or a phenyl group substituted by lower alkyl group, lower alkoxy group, halogen atom, or lower haloalkyl group.

Abstract: An efficient protocol for the synthesis of taxol, taxol analogs and their intermediates is described. The process incudes the attachment of the taxol A-ring side chain to baccatin III and for the synthesis of taxol and taxol analogs with variable A-ring side chain structures. A rapid and highly efficient esterification of O-protected isoserine and 3-phenylisoserine acids having N-benzyoloxycarbonyl groups to the C-13 hydroxyl of 7-O-protected baccatin III is followed by a deprotection-acylation sequence to make taxol, cephalomanninne and various analogs, including photoaffinity labeling candidates.

Abstract: A process for preparing N-acyl, N-sulfonyl and N-phosphoryl substituted isoserine esters in which a metal alkoxide is reacted with a .beta.-lactam.