Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are as defined in the specification as well as to the novel intermediates obtained by said process.

Abstract: Onium salts of taxo-diterpenoid-Cn,2-O-aza-arenes form water soluble self-assembling nanostructures above a critical aggregation concentration. The onium salt of aza-arene includes a delocalized charge which renders derivatized taxo-diterpenoids amphoteric, enhances their solubility in water, and promotes self-assembly of water soluble nanostructures, e.g., helical fibular structures and spherical micellular structures. These same onium salts of taxo-diterpenoid-Cn,2-O-aza-arenes are employed as water soluble prodrugs. For example, taxol-2′-methylpyridinium tosylate (MPT) is characterized by an elevated aqueous solubility, rapid activation by serum protein, good stability in most other aqueous solutions, formation of a protein:taxol intermediate and good retention within the circulatory system. The toxicity of the activated form is comparable or greater than underivatized taxol. Furthermore, taxol-2′-MPT can be synthesized by a simple one step reaction between taxol and 2-fluoro-1-MPT.

Abstract: The use of nitroethane derivatives of the formula I where: R1 is hydrogen, unsubstituted or substituted C1-C6-alkyl, C3-C6-alkenyl, C3-C6-alkynyl, halogen, cyano or thiocyanato; R2 is hydrogen, formyl; halogen- or C1-C3-alkoxy-substituted or unsubstituted C1-C6-alkylcarbonyl, C2-C6-alkenylcarbonyl, C4-C6-alkyldienylcarbonyl or C2-C6-alkynylcarbonyl; A is unsubstituted or substituted phenyl, naphthyl, quinolyl, quinazolyl, quinoxalyl, 1-methylindolyl, 1-methylbenzimidazolyl, 2-methylindazolyl, benzofuranyl, benzothienyl, benzoxazolyl, benzothiazolyl, furyl, thienyl, pyrrolyl, isoxazolyl, isothiazolyl, pyrazolyl, oxazolyl, thiazolyl, imidazolyl, oxadiazolyl, thiadiazolyl, triazolyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl or triazinyl, pyranyl or thiopyranyl; as microbicides is described.

Abstract: A process for the continuous production of 1,3-dioxolan-2-ones such as ethylene carbonate or propylene carbonate by reacting a corresponding oxirane with carbon dioxide in the liquid phase in the presence of a catalyst comprises conducting the reaction in a two-part reactor in whose first part the reaction is taken with backmixing to a conversion of not less than 80% of the oxirane II and in whose second part the reaction is completed under nonbackmixing conditions, and passing the carbon dioxide in countercurrent to the oxirane II in the entire reactor.

Abstract: The present invention relates to new intermediates for the semisynthesis of taxanes and their preparation processes. It relates to derivatives of oxazolidines or oxazolidinones, as well as to new derivatives of baccatine III. The general process for the synthesis of taxanes according to the invention enables to obtain a product such as PACLITAXEL in only five steps from products available in the market, compared to nine steps in general, for processes of the prior art.

Abstract: The present invention relates to chemical compounds that are useful in the production of taxanes. The chemical compounds according to the present invention have a generalized formula: wherein R1 is NH2, and wherein R2 may be acetyl or hydrogen, and p1 may be hydrogen or a hydroxyl protecting group.

Abstract: The invention relates to modified benzylidene-&ggr;-butyrolactones, to a process for their preparation and to the use as UV absorber, for example in pharmaceutical and cosmetic compositions, sunscreens, daycare and haircare products, for improving industrial products, such as paints, surface coatings, plastics, textiles, packaging materials and rubbers.

Abstract: A process and catalyst for the hydro-oxidation of an olefin having three or more carbon atoms, such as propylene, to form an olefin oxide, such as propylene oxide. The process involves contacting the olefin with oxygen under reaction conditions in the presence of hydrogen and a catalyst. The catalyst contains oxidized gold dispersed on a titanium-containing support, preferably, a support having a plurality of titanium coordination environments, for example, titanium grafted onto a titanosilicate. Selectivity to olefin oxide is high at good conversion of the olefin. The catalyst uses hydrogen efficiently and exhibits a long lifetime.

Abstract: A compound of formula (IV): wherein R′ and R9 are each independently (C1-C4)alkyl.

Abstract: Cyclic chemical switching method is employed for solubilizing and desolubilizing taxo-diterpenoids with respect to aqueous solvents. 2-Halogenated onium salts of aza-arenes are employed to derivatize taxo-diterpenoids so as to alter their solubility in aqueous solvents. The onium salt of aza-arene includes a delocalized charge which imparts polarity and aqueous solubility to taxo-diterpenoid derivatives. Solubilization is achieved in a one step derivatization with the onium salt of 2-halogenated aza-arenes. Desolubilization is achieved by contacting onium salts of taxo-diterpenoid-Cn,2-O-aza-arenes with serum protein to displace the 2-O-aza-arene and form a soluble protein:taxo-diterpenoid intermediate. This protein:taxo-diterpenoid intermediate then dissociates over time to provide a bioactive taxo-diterpenoid. These same onium salts of taxo-diterpenoid-Cn,2-O-aza-arenes are employed as water soluble prodrugs. The toxicity of the activated form is comparable or greater than underivatized taxol.

Abstract: Method of producing an antitumor preparation of natural origin lyophilized arglabin 1&bgr;, 10&bgr;-epoxy-13-dimethylamino-guaia-3(4)-en-6, 12-olide hydrochloride includes resin extraction from a natural material, its purification from worthless substances, resin separation into separate components by column chromatography with production of technical arglabin. Technical arglabin further undergoes recrystallization, amination and hydrochloration at given parameters of pH solutions with production of aminoarglabin hydrochloride and its further lyophilization and high quality identification by IR-spectroscopy. A device for the realization of the method is also disclosed herein.

Abstract: Invention relates to H2S scavengers polysulfide compounds and methods for scavenging H2S from polysulfide compounds. Furthermore, the invention uses a scavenger for selectively reducing the levels of hydrogen sulfide present in a polysulfide product.

Abstract: Dikegulac, its salts and related derivatives are prepared by reacting 2-Keto-L-gulonic acid with 2,2 dimethoxypropane at an elevated temperature in the presence of a catalytic amount of a strong acid. This produces a reaction intermediate which is then reacted with a base to complete hydrolysis and produce an acid salt of dikegulac. Simple concentration and phase separation techniques are used to provide a more efficient, environmentally friendly and cost effective process.

Abstract: Methods of preparing new taxoids of general formula (I) are presented: in which: R4 represents an alkanoyloxy radical in which the alkanoyl portion contains 2 to 6 carbon atoms in an unbranched or branched chain, this radical unsubstituted or substituted with one or more halogen atoms, an alkoxy radical containing 1 to 4 carbon atoms, or alternatively R4 represents a cycloalkanoyloxy radical in which the cycloalkanoyl portion contains 4 to 8 carbon atoms, or alternatively R4 represents a benzoyloxy radical; R5 represents an alkoxy radical containing 1 to 4 carbon atoms, substituted by an alkylthio radical containing 1 to 4 carbon atoms; and Z represents a hydrogen atom or a radical of general formula:

Abstract: The invention provides a process for the catalytic epoxidation of alkene comprising contacting a transition metal substituted polyoxometalate and molecular oxygen with alkene.

Abstract: The object of the present invention is the development of new chiral auxiliaries for improved &bgr;-lactam formation that control both the diastereoselectivity of &bgr;-lactam formation and which can be removed without destruction of the sensitive azetidinone ring, providing valuable intermediates for coupling to the C-13 hydroxyl group of anti-tumor taxanes, such as paclitaxel. Further, the object of the present invention is enantiomerically pure (S)-(−)-1-(p-methoxy-phenyl)propyl-1-amine.

Abstract: Provided by the invention is a chemical-amplification positive-working photoresist composition used in the fine photolithographic patterning in the manufacturing process of semiconductor devices, which is suitable for the patterning light exposure with ArF excimer laser beams of very short wavelength by virtue of absence of aromatic structure in the ingredients of the composition. The composition comprises, as the film-forming resinous ingredient, an acrylic resin having unique monomeric units represented by the general formula &Brketopenst;CH2—CR1(—CO—O—CR2R3R4)&Brketclosest;, in which R1 is a hydrogen atom or a methyl group, R2 and R3 are each, independently from the other, an alkyl group having 1 to 4 carbon atoms and R4 is an alkoxycarbonyl group or a group derived from a molecule of a lactone compound or ketone compound by removing a hydrogen atom bonded to the carbon atom.

Abstract: The present invention relates to the use of known efomycins and elaiophylins for the treatment of autoimmune disorders, to new natural substances efomycins M and T, and processes for their preparation; in particular to their use as medicaments in psoriasis therapy.

Abstract: The present invention relates to a semi-synthetic process to convert a naturally occurring taxane into a suitable starting material for the synthesis of paclitaxel and related compounds. Specifically, the present invention relates to a process for the conversion of 9-dihydro-13-acetylbaccatin III into a 7-protected baccatin III which can then be used as starting material for the synthesis of taxane derivatives such as paclitaxel, docetaxel, cephalomannine and other taxanes structurally related to baccatin III. The method as described uses a preparative scale technique which is amenable to commercial scale-up.

Abstract: The method for producing an epoxy resin involving the steps of: reacting at least one phenol compound with at least one aldehyde compound to obtain a novolak resin; storing the novolak resin in a molten state in an inert gas atmosphere; feeding the stored novolak resin into an epoxidation reactor; and reacting the stored novolak resin with an epihalohydrin compound, which prevents generation of dust improving the working environment, increases production efficiency reducing production cost, and further suppresses quality degradation such as coloring of the epoxy resin.