Abstract: Taxane derivatives modified at 13-position of the taxane derivative skeleton (taxol numbering) of formula (I), wherein R, R.sub.a, R.sub.b, R.sub.c, R.sub.1, R.sub.2, R.sub.3 are appropriate organic residues can be antitumor agents.

Abstract: Propylene is converted to propylene oxide in a highly efficient liquid phase process wherein temperature and pressure are both increased over the course of the epoxidation, which is preferably conducted in a continuous mode of operation. The catalyst used is a heterogeneous catalyst such as titanium silicalite or titania-on-silica. The oxidizing agent is an active oxygen species such as hydrogen peroxide or an organic hydroperoxide. When the desired yield of propylene oxide can no longer be maintained, the catalyst is replaced or regenerated.

Abstract: The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.

Abstract: Method which includes passing a gas stream containing carbon dioxide, hydrogen sulfide, sulfur dioxide, mercaptans and other acid gases through an aqueous alkanolamine solution to remove the carbon dioxide, hydrogen sulfide, sulfur dioxide, mercaptans, etc., from the gaseous stream. Heat-stable alkanolamine salts form in the aqueous alkanolamine solution due to the acid contaminants (other than hydrogen sulfide or carbon dioxide) removed from the gas stream. A base is added to the aqueous alkanolamine solution to convert all or part of the heat-stable alkanolamine salts into alkanolamine and simple salts. The base-treated aqueous alkanolamine solution is electrodialyzed in an electrodialysis cell containing ion exchange membranes. The purified aqueous alkanolamine solution can be used again to remove carbon dioxide, etc., from the gas stream.

Abstract: Epoxy-containing compounds which are essentially free of organic halides are prepared by (I) reacting an allyl derivative of an active hydrogen-containing compound with (II) a peroxygen-containing compound. The epoxy-containing compounds are useful in coatings, castings, laminates etc.

Abstract: Process for regenerating a silver catalyst deactivated by coking during the gas phase epoxidation of 1,3-butadiene by reacting the coked catalyst with a gas mixture containing at least 5% by volume of water vapor and up to 95% by volume of oxygen at temperatures of from 100 to 500 .degree. C.

Abstract: The epoxidation is carried out in a reaction system made of metal under conditions such that the inner surface area (S) of the reaction system exposed to the gaseous-phase part thereof and the amount of the reaction solution (V) in the reaction system satisfy the formula: 0<S/V.ltoreq.2 (m.sup.2 /m.sup.3). The epoxidation, otherwise, is carried out in a reaction vessel such that at least the inner surface thereof exposed to the gaseous-phase part thereof has been inactivated or in a reaction vessel such that at least the inner surface thereof exposed to the gaseous-phase part thereof has been inactivated. A hydroxy iminodisuccinic acid is produced by causing the epoxysuccinic acid which has been obtained as described above to react with L-aspartic acid. By this reaction, an epoxy compound can be produced with a high yield without inducing coloration by epoxidizing a corresponding ethylenic compound with hydrogen peroxide.

Abstract: L-ascorbic acid is produced by allowing an acid to act on 2-keto-L-gulonic acid in a mixture solvent of an inert organic solvent and an aliphatic ketone in the presence of water and a surfactant.The method produces L-ascorbic acid in a high yield 90% or more and is an industrially advantageous method.

Abstract: Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.

Abstract: A method is described for the synthesis of oxetan-2-ones comprising protection of the hydroxy group of an hydroxy ester with an acid-labile acetal protecting group, reduction of this O-protected hydroxy ester to an O-protected hydroxy aldehyde, condensation of this aldehyde with a metal enolate of an activated carboxylic acid derivative and spontaneous deprotection of the hydroxy group during the acidic workup procedure. Using the new O-protected hydroxy aldehydes as intermediates the oxetan-2-ones can be obtained after separation in diastereomerically and enantiomerically pure form, in a remarkably reduced number of steps, and in a significantly improved overall yield.

Abstract: The present invention concerns novel paclitaxel derivatives, their use as antitumor agents, and pharmaceutical formulations.

Abstract: A process for the manufacture of d,l-.alpha.-tocopherol by condensing trimethylhydroquinone with isophytol comprises carrying out the condensation in the presence of a polyperfluoroalkylenesulphonic acid as the catalyst and in a solvent, especially an aprotic solvent. The catalyst is preferably a polyperfluoroalkylenesulphonic acid from the Nafion.RTM. series, e.g., Nafion NR 50.RTM. or Nafion 117.RTM..

Abstract: Cyclic cedrene acetals of the general formula A are described, in which the wavy lines represent the .alpha.- and .beta.-configurations, and R and R.sub.1 are the radicals below: ##STR1## R=R.sub.1 =H R=H, R.sub.1 =Me/R=Me, R.sub.1 =HR=H, R.sub.1 =Et/R=Et, R.sub.1 =HR=H, R.sub.1 =Pr/R=Pr, R.sub.1 =HR=H, R.sub.1 =Bu/R=Bu, R.sub.1 =HR=H, R.sub.1 =Iso-Bu/R=Iso-Bu, R.sub.1 =HR=H, R.sub.1 =Pentyl/R=Pentyl, R.sub.1 =HR=H, R.sub.1 =Iso-Pentyl/R=Iso-Pentyl, R.sub.1 =HR=H, R.sub.1 =Hexyl/R=Hexyl, R.sub.1 =HR=R.sub.1 =Me (.alpha.,.beta.)R=Me, R.sub.1 =Fl/R=Et, R.sub.1 =MeR=R.sub.1 =Fl (.alpha.,.beta.)R=Me, R.sub.1 =Pr/R=Pr, R.sub.1 =MeR=Pt, R.sub.1 =Pr/R=Pr, R=EtR=R.sub.1 =CyclobutylR=R.sub.1 =CyclopentylR=R.sub.1 =Cyclohexyl.

Abstract: An antitumor compound of formula (5) ##STR1## in which R is Ac or H, and R.sub.1, R.sub.2 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.3 is H; R.sub.1 and R.sub.2 and R.sub.3 are H; R.sub.1 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R.sub.2, R.sub.3 is H; R.sub.1 and R.sub.3 are H, R.sub.2 is an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 is H, R.sub.2 and R.sub.3 are an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R.sub.1 and R.sub.2 and R.sub.3 are an alkyl group Me, Et, Pr, i-Pr, n-Bu or t-Bu. Me is an abbreviation for methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, n-Bu is n-butyl, and t-Bu is tert-butyl. Also provided by the invention is a one step method of preparing a compound of formula (5) whereby a taxane having a tiglate group attached to the side chain is contacted with an oxidizing reagent resulting in the formation of an epoxide having antitumor activity.

Abstract: Disclosed is an improved process for the catalytic hydrogenation of cyanopropionaldehyde alkyl acetals (CPAA) to form the aminobutyraldehyde alkyl acetals. The basic process comprises hydrogenating the cyanopropionaldehyde alkyl acetals by contacting said cyanopropionaldehyde alkyl acetals with hydrogen in the presence of a nickel or cobalt catalyst under conditions for reducing the nitrile group to the primary amine. The improvement resides in effecting the hydrogenation of a cyanopropionitrile dialkyl acetal feedstock containing contaminating levels of cyanopropionaldehyde in the presence of a secondary alkanol or water.

Abstract: Process for preparing optically active trans-3-phenylglycidamide compound, which comprises subjecting racemic trans-3-phenylglycidamide compound of the formula (I) ##STR1## wherein Ring A is substituted or unsubstituted benzene, and R.sup.1 is H or lower alkyl, to optical resolution using a microorganism having ability of preferentially hydrolyzing one of (2S,3R) isomer or (2R,3S) isomer thereof, and process for preparing an optically active 1,5-benzothiazepine derivative from the thus-obtained optically active trans-3-phenylglycidamide compound.

Abstract: The invention relates an epoxysuccinamide derivative represented by the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different from each other and independently represent H or an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring together with the adjacent nitrogen atoms, R.sup.3 is H or an acyl group, R.sup.4 is H or an aralkyl group, and R.sup.5 is an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.5 may form an amino acid residue, which may be protected, together with the adjacent nitrogen atom, or a salt thereof, and a medicine comprising the derivative as an active ingredient; and this compound has an inhibiting activity against cathepsin, and particularly, specifically inhibits cathepsin L and is hence useful for prevention and treatment of osteopathy such as osteoporosis.

Abstract: High molecular weight, water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active moiety;M is X or Q;X is an electron withdrawing group;Q is a moiety containing a free electron pair positioned five or six atoms from Y';Y and Y' are oxygen or sulfur;R is a polyalkylene oxide; andZ is OH, C.sub.1-4 all moieties or ##STR2## are disclosed. In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.

Abstract: A process for the distillation of the glycidyl ester reaction product of a straight or branched chain saturated monocarboxylic acid or salt thereof and an halo-substituted monoepoxidc is disclosed, wherein the reaction product is subjected to conditions of temperature and vacuum in a thin film, short pass distillation apparatus such as a wiped film evaporator. The product distillate has significantly reduced color than the reaction product prior to distillation, and has improved heat and color stability.

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.