Abstract: The present invention relates to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, more particularly to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, a novel compound having the structure represented by the following Chemical Formula 1, from trimethylsilanylmethyl-allenol derivative by the intramolecular Prins cyclization using Lewis acid. The 8-membered carbocyclic compound is a useful intermediate for synthesis of other multicarbocyclic compounds. In Chemical Formula 1, R1 is a phenyl group, and R2 and R3 is a hydrogen atom, or R1, R2 and R3 may be connected with neighboring substituents to form a 5 to 10-membered aliphatic or aromatic ring.

Abstract: The present invention describes novel nitrosated and/or nitrosylated taxanes, and novel compositions comprising at least one nitrosated and/or nitrosylated taxane, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The present invention also provides novel compositions comprising at least one taxane and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The compounds and compositions of the present invention can also be bound to a matrix.

Abstract: A continuous and scalable process for producing glycidyl nitrate, or glyn, from glycerin, nitric acid, and caustic wherein the process includes the reaction of glycerin and nitric acid to form dinitroglycerin and the reaction of dinitroglycerin with caustic, such as sodium hydroxide, system for producing the inventive material is also disclosed. The vessel, a second reaction vessel, and a separation apparatus.

Abstract: Methods for manufacture of citalopram through stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans are disclosed.

Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.

Abstract: A process is provided in which at least one multi-functional alcohol having a hydroxyl functionality of at least two serves as a polymerization initiator. The multi-functional alcohol initiator is optionally, although preferably, reacted with a catalyst to form a catalyst-initiator complex, which is then used in the polymerization of glycidyl nitrate. The resulting poly(glycidyl nitrate) has a functionality substantially equivalent in number to the hydroxyl functionality of the multi-functional alcohol initiator. The poly(glycidyl nitrate) is cross-linked with at least one aromatic polyisocyanate having at least one aromatic ring and, on average, more than two isocyanate moieties bonded directly to the aromatic ring.

Abstract: The synthesis of taxol and other tricyclic and tetracyclic taxanes.

Abstract: The object of the present invention is to provide a novel method for effectively producing a cyclic lactic acid oligomer, and a cyclic lactic acid oligomer produced by the method.

Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.

Abstract: Novel derivatives of isosorbide mononitrate and its pharmaceutically acceptable salts, which have vasodilating activity with a reduced effect of tolerance, of the general formula (I) in which A and B independently represent any of the groups —ONO2 and —Z—CO—R, wherein Z is an oxygen atom or sulphur atom and R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, or the group in which R1 is hydrogen, or an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, with the proviso that one of A or B is always —ONO2, but never both of them at the same time, when Z is an sulphur atom R is an alkyl C1-C4 group, an aryl group or an aralkyl group, eventually substituted, and when Z is an oxygen atom R is the group

Abstract: The invention relates to a method for the production of 2-coumarone or substituted 2-coumarones, whereby cyclohexanone or substituted cyclohexanone is reacted with a carboxyl-containing acylating agent a) to give methyl 2-(2-oxo-cyclohexyl)-2-hydroxyacetate or substituted methyl 2-(2-oxo-cyclohexyl)-2-hydroxyacetates, which are either a1) directly converted to 2-coumarone or substituted 2-coumarones by means of catalytic gas-phase dehydrogenation, or a2) dehydrated by means of azeotropic distillation under basic conditions, or by use of a strong acid, or a strongly acidic ion exchanger to a mixture of methyl 2-oxocyclohexylidenacetate and the enol-lactone of the 2-oxocyclohexylidenacetic acid, or a mixture of substituted methyl 2-oxocyclohexylidenacetate and the enol-lactone of the substituted 2-oxocyclohexylidenacetic acid, which is finally converted in turn by catalytic gas-phase dehydrogenation to 2-coumarone, or substituted 2-coumarones, or b) are directly converted under acidic or basic conditions into a

Abstract: Allomorph of Z isomer of N-[2-[[[5-(dimethylamino)methyl-2-furanyl]methyl]thio]ethyl]-N?-methyl-2-nitro-1,1-ethenediamine hydrochloride, with two carbon atoms linked by a rigid ethylenic bond, marked by an asterisk (*), characterized by the following structural formula: wherein -Fur- represents a furane ring.

Abstract: Processes are disclosed for the preparation of 2-methylfuran and 2-methyltetrahydrofuran. The continuous vapor-phase processes are commercially viable and efficient because they permit the preparation of 2-methylfuran and 2-methyltetrahydrofuran using commercially-available catalysts, namely, a reduced copper-based catalyst consisting essentially of cupric oxide, chromium (III) oxide, manganese oxide and barium chromate and a reduced nickel-based catalyst consisting essentially of nickel, nickel (II) oxide, aluminum oxide and silica. An apparatus comprising two inline hydrogenators is used for preparing the 2-methylfuran or 2-methyltetrahydrofuran.

Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.

Abstract: A method for removing acyl-groups appended by an ester linkage to the 2?-hydroxyl group present in paclitaxel-related molecules comprising treatment with alcohol under non-acidic conditions.

Abstract: A method of isolating terpene trilactones from Ginkgo biloba plant material or extract comprising the steps of suspending the plant material or extract in either water or an aqueous solution of an oxidation reagent; extracting the terpene trilactones using an acceptable extraction agent; separating the organic layer from the aqueous layer; washing the organic layer with an acceptable aqueous salt or hydroxide solution, which may be an alkaline solution; and drying the organic layer to form a dried extract containing terpene trilactones. Further purification by treatment with or filtration over activated charcoal, by treatment with or filtration over alumina and by recrystallization with an acceptable solvent or solvent mixture leads to extracts with a content of terpene trilactones higher than 50%. Unwanted levels of ginkgolic acids are reduced to acceptable levels by reversed phase chromatography.

Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.

Abstract: Process for manufacturing oxirane by reaction of an olefin with a peroxide compound in the presence of a catalyst and a solvent in at least two reactors arranged in series, each of which contains a portion of catalyst, according to which the peroxide compound is introduced only into the first reactor, the subsequent reactor(s) not being fed with fresh peroxide compound, but only with the peroxide compound which is present in the medium obtained from the preceding reactor and which was not consumed in this preceding reactor.

Abstract: The invention relates to the synthesis of alkenoate esters from a corresponding lactone and an alcohol in the presence of a basic catalyst. More specifically, this invention relates to the synthesis of methyl-4-pentenoate ester from 5-methyl butyrolactone and methanol.

Abstract: Pharmaceutical compositions, methods of administration, and methods of treatment of cancer with new generation taxoids, of formulas (I) and (II), and derivatives thereof, are described: