Abstract: The invention provides substituted furanone antiarthritic and analgesic pharmaceutical agents defined by Formula I, ##STR1## wherein: R.sup.1 is selected from the group consisting of(a) S(O).sub.2 CH.sub.3,(b) S(O).sub.2 NH.sub.2,(c) S(O).sub.2 NHC(O)CF.sub.3,(d) S(O)(NH)CH.sub.3,(e) S(O)(NH)NH.sub.2,(f) S(O)(NH)NHC(O)CF.sub.3,(g) P(O)(CH.sub.3)OH, and(h) P(O)(CH.sub.3)NH.sub.2 ;R.sup.2 and R.sup.3 independently are selected from(1) hydrogen,(2) halo,(3) C.sub.1 -C.sub.6 alkyl,(4) C.sub.1 -C.sub.6 alkoxy, and(5) C.sub.1 -C.sub.6 alkylthio;n is an integer from 1 to 3;m is an integor from 1 to 3;or a pharmaceutically acceptable salt thereof.

Abstract: A derivative or analog of baccatin III or 10-desacetyl baccatin III having a C-9 substituent other than keto.

Abstract: It has been surprisingly discovered that the disadvantages of the lengthy literature procedures to synthesize 13,14-dihydro prostaglandin A, E, and F derivatives can be overcome using a novel Methyl 7-(2-hydroxy-5-(2-(2-oxiranyl)ethyl)-4-(1,1,2,2 tetramethyl-1-silapropoxy)cyclopentyl) heptanoate intermediate, which can be synthesized from commercially available Methyl 7-[3-(R)-hydroxy-5-oxo-1-cyclopent-1-yl] heptanoate. This novel intermediate can be coupled with oxygen, carbon, sulfur, and nitrogen nucleophiles, in the presence of a base or a Lewis acid, in a ring-opening process to provide 13,14-dihydro prostaglandin A, E, and F derivatives.

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. Regeneration by washing the catalyst with a hot solvent containing a source of ammonium or alkali metal cations is highly effective, especially where the catalyst is a titanium-containing zeolite.

Abstract: The present invention teaches a method of extracting TAXOL.RTM. from the leaves of taxus cupidata plants. The process comprises a series of steps, including the concentration of the extracts obtained from the plant, the separation of the aqueous and chloroform phases, and several purification procedures. In addition, the present invention teaches a multi-step process wherein the virtual removal of chlorophyll is achieved prior to the introduction of the extract into the silica gel packing material. This prevents the deactivation of the silica gel packing material by chlorophyll in the extract solution.

Abstract: A method of acylating C-2' O-protected-10-hydroxy taxol selectively at the C-10 hydroxyl position over the C-7 hydroxy position thereof to produce C-2' O-protected taxol is accomplished first by dissolving C-2' O-protected-10-hydroxy taxol in an acceptable ether solvent therefor, such as tetrahydrofuran, to form a first solution at a first temperature. The first solution is then cooled to a second temperature, and a lithium base, preferably n-butyl lithium, is added to form an intermediate compound having a lithium alkoxide at the C-10 position thereof. An acylating agent, such as acetyl chloride, is then added. The resulting solution may be quenched, for example with ammonium chloride, to eliminate excess of the acylating agent and the lithium base. The result is a solution containing C-2' O-protected taxol. This solution may then be washed, concentrated and purified. The present invention is also directed to C-10 lithium alkoxide intermediate compounds for the production of paclitaxel.

Abstract: The present invention relates to a heterogeneous polyimide-supported transition metal complex catalyst for epoxidation of olefin, which is prepared by impregnating a heat- and acid-resistant polyimide resin with a homogeneous metal catalyst of molybdenum, vanadium, tungsten or titanium, and a process for preparing epoxy compounds using the same. The heterogeneous polyimide-supported transition metal complex catalyst of the invention provides superior catalytic activity, selectivity and stability in the epoxidation of higher olefin. Further, the catalyst of the invention has strong resistance against heat and acid. Besides, the catalyst of the invention may provide the following advantages which are critical in industrial use: it permits relatively high yield of epoxy compounds; and, it can be easily separated from the reaction product, which eases recycling of the catalyst.

Abstract: Process for the production of epoxides by reaction between 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 treatment with organic molecules comprising an amide group substituted on the nitrogen atom.

Abstract: To provide an epoxy resin composition which can provide a cured resin which is excellent in weatherability and electric properties, and which is useful as a resin for coatings, an encapsulant, a casting material, an electric insulator, etc. An epoxy resin composition which contains a hydrogenated epoxy resin obtained by hydrogenation of an aromatic epoxy resin, wherein the hydrogenated epoxy resin has a hydrogenation ratio in an aromatic ring of not less than 85%, a loss ratio of epoxy groups of not more than 20%, and a total chlorine content of not more than 0.3% by weight.

Abstract: Spontaneously dispersible concentrates comprising new esters of Baccatin-III, 10-Deacetylbaccatin-III and 14-OH-10-Deacetylbaccatin-III, procedures for their production. The preparation of aqueous ultramicroemulsions, their incorporation into pharmaceutical compositions having antitumor, antiviral and virucidal activity, are efficacious in the treatment of eczemae and psoriasis and stimulate the increased absorption of exogenous activators, regulators or modulators, are described.

Abstract: The present invention provides a process for producing an optically active aldehyde which comprises hydroformylating a terminal olefin substrate represented by the formula:Q.sub.1 Q.sub.2 C.dbd.CH.sub.2wherein Q.sub.1 is an atom or group other than carbon or hydrogen and Q.sub.2 is an atom or group other than hydrogen, in the presence of CO, H.sub.2 and a catalyst, which catalyst comprises a transition metal based compound and a ligand.

Abstract: The invention concerns novel bi-aromatic dibenzofuran derivatives of formula (I),and their use in pharmaceutical compositions for human or veterinary medicine (skin, rheumatic respiratory, cardiovascular, and ophthalmologic disorders), or in cosmetic compositions as well. The X, Ar, R.sub.1 and R.sub.2 in formula (I) are defined in the specification.

Abstract: Reacting a diol (1) with a carbonic ester (2) to produce a cyclic carbonic ester (3) using a salt of a weak acid with an alkaline metal or alkaline earth metal as a catalyst. The diol (1) contains diols having an asymmetric carbon atom. The reaction mixture is neutralized and distilled to obtain a cyclic carbonic ester. Cyclic carbonic esters are produced using an easily accessible and easy to handle reactant, with good yield and under mild and moderate conditions.

Abstract: Unsaturated or polyunsaturated, conjugated or nonconjugated hydrocarbons are reacted with an oxidizing agent including hydroperoxides and monopersulfate compounds in the presence of phase-transfer catalysts. Suitable hydrocarbons include ricinic compounds such as castor oil and dehydrated castor oil. The phase-transfer catalysts include novel tungsten peroxo complexes, such as quaternary ammonium tetrakis (diperoxotungsto) phosphates, and crown ethers. Other additives opionally utilized include pH buffers, alkaline compounds, and solvents.

Abstract: Taxane derivatives having an amino substituted C13 side chain.

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"). 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.

Abstract: A process of preparing ring E-modified analogues of (-)-podophyllotoxin as potential new chemotherapeutic agents. The process generates corresponding analogues of (-)-podophyllotoxin, itself, and allows new molecular interactions in the southern hemisphere (ring E) of the molecule. A method of preparing enantiomerically enriched compounds of the formula (I) and (II): ##STR1## wherein R is: ##STR2## wherein X, X', Y, Y' and Z are ring E substituents and R.sup.1 is one of a)-e) below.a) --OH,b) an ether or glycoside,c) a substituted or unsubstituted amine or aniline,d) a C.sub.2 -C.sub.8 alkenyl group, preferably --CH.sub.2 CH.dbd.CH.sub.2,e) a C.sub.1 -C.sub.8 alcohol, preferably --CH.sub.2 CH.sub.2 CH.sub.2 OH.The process produces enantiomerically enriched compounds which do not occur naturally and are not readily available from (-)-podophyllotoxin.

Abstract: A method of acylating C-2' O-protected-10-hydroxy taxol selectively at the C-10 hydroxyl position over the C-7 hydroxy position thereof to produce C-2' O-protected taxol is accomplished first by dissolving C-2' O-protected-10-hydroxy taxol in an acceptable ether solvent therefor, such as tetrahydrofuran. A lithium salt, preferably lithium chloride, is added. A trialkylamine base or pyridine is next added, followed by the addition of an acylating agent, such as acetyl chloride. The resulting solution may be quenched, for example with ammonium chloride, to eliminate excess of the acylating agent. This solution may then be diluted with ethyl acetate to form an organic phase and an aqueous phase, with the organic phase being washed and thereafter reduced. Recrystallization and column chromatography may be employed to purify the C-2' O-protected taxol.

Abstract: Alpha-hydroxy-epoxides of alpha-alkoxy-epoxides of the formula IV ##STR1## in which the substituents have the following meanings: R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 are independently hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.3 -C.sub.12 -cycloalkyl, C.sub.4 -C.sub.20 -cycloalkylalkyl, C.sub.1 -C.sub.20 -hydroxy-alkyl, a heterocyclic ring, or an aryl or C.sub.7 -C.sub.20 -arylalkyl group optionally substituted by C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, halogen, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -halo-alkoxy, phenyl, phenoxy, halophenyl, halophenoxy, carboxy, C.sub.2 -C.sub.8 -alkoxycarbonyl, or cyano, or R.sup.7 and R.sup.8 or R.sup.7 and R.sup.9 or R.sup.7 and R.sup.10 or R.sup.9 and R.sup.10 or R.sup.10 and R.sup.11 together form a (CH.sub.2).sub.n group in which n is an integer from 1 to 10 and which may be optionally substituted by C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, and/or halogen, andR.sup.12 is hydrogen, C.sub.1 -C.sub.8 -alkyl, or benzyl,provided that R.

Abstract: A method for esterifying C13 deoxy taxoid intermediates employs three steps, i.e., oxygenation of the C13 deoxy taxoid intermediate to produce a C13 enone taxoid intermediate; reduction of the C13 enone to produce an alcohol; followed by esterification of the C13 alcohol. Key intermediates include C13 deoxy taxoids; C13 enone substituted taxoids; and C1-C2 cyclo carbonate esters of taxoids.