Abstract: A process for the preparation of novel C-4 carbonate taxanes useful as antitumor agents

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

Abstract: A material especially useful for the selective oxidation of hydrocarbons and other organic compounds includes a non-crystalline, porous inorganic oxide having at least 97 volume percent mesopores based on micropores and mesopores, and at least one catalytically active metal selected from the group consisting of one or more transition metal and one or more noble metal.

Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably substituted at the 4-position. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

Abstract: A process for purifying propylene oxide containing an unacceptable quantity of a poly (propylene oxide) polymer contaminant having a number average molecular weight of at least 50,000 and precursors having a number average molecular weight below 50,000. The process comprises contacting the propylene oxide with a sorbent selected from activated carbon, charcoal, and attapulgite for a time and under conditions sufficient to reduce the amount of the contaminant to acceptable levels, and thereafter recovering the purified propylene oxide product, wherein the propylene oxide is contacted with the sorbent at a temperature below 10° C.

Abstract: Methods for obtaining bryostatins from the marine bryozoans of the Bugula neritina species complex are provided wherein the methods involve the extraction and purification of bryostatins from the larvae of Bugula neritina organisms. Further, the present invention relates to a novel bryostatin composition that can be extracted from Bugula neritina.

Abstract: Compounds of Formula Ia and Ic having a lactone structure and an methylene group at the alpha-position of the lactone structure and methods for using and making the compounds have been disclosed. The lactone compounds can be reacted with an neucleaphilic agent to open the lactone ring to a compound of Formula Ib. The lactone of Formula Ia and its functional derivatives have been isolated from Securidaca virgata. These compounds are referred to as LMSV-6 or Securolide™. The purified compounds have demonstrated activity in assays for anti-bacterial and anti-fungal activities, and for treating proliferation disorders such as cancer. Based on the in vitro assays, the lactones are useful for treating proliferation disorders including, for example, breast cancer, colon cancer, rectal cancer, stomach cancer, pancreatic cancer, lung cancer, liver cancer, ovarian cancer, esophageal cancer, and leukemia.

Abstract: A method of producing an N-alkoxycarbonylpiperidine derivative, comprising reacting an N-aralkylpiperidine derivative represented by the following general formula (1): wherein R1 represents an aralkyl group which may have a substituent, with a mesyl halide in the presence of a base, thereby obtaining a mesylated product represented by the following general formula (2): wherein R1 represents an aralkyl group which may have a substituent and Ms represents a mesyl group, and reacting the mesylated product with a dicarbonate represented by the following general formula (3): wherein R4 represents an alkyl group, in the presence of hydrogen and a catalyst containing palladium, thereby obtaining an N-alkoxycarbonylpiperidine derivative represented by the following general formula (4): wherein R4 represents an alkyl group and Ms represents a mesyl group.

Abstract: For the preparation of an 11-oxaprostaglandin such as [2R,(1E,3R),3S,(4Z),4R)]-7-{tetrahydro-2-[4-(3-chlorophenoxy)-3-hydroxy-1-butenyl]-4-hydroxy-3-furanyl}-4-heptenoic acid and its ester derivatives, a novel process uses a novel enantiomerically enriched compound for formula (1) wherein the bond between carbon atoms y and z is either a single or double bond; R1 is selected from vinyl, trialkylsilylethynyl, a formyl group protected as an acetal, or a protected hydroxymethyl group; R2 is C1-5 alkyl, optionally substituted at the terminus with an aryloxy or alkoxy group; and R3-R6 are independently selected from C1-6 alkyl and C6-10 aryl

Abstract: A process for the preparation of taxanes including paclitaxel, docetaxel, and structurally similar analogs, as well as intermediates produced by the process.

Abstract: A process for the purification of paclitaxel or docetaxel comprising: (a) mixing crude paclitaxel with a mixture of solvents such as alkane and chlorinated alkane, filtering the solid followed by drying to obtain paclitaxel or docetaxel of increased purity; (b) repeating step (a) one or more times to obtain paclitaxel or docetaxel of increased purity; (c) dissolving the solid obtained from step (b) in alkyl ketone followed by adding alkane thereto, filtering and drying the solid thus formed to obtain paclitaxel or docetaxel of increased purity; (d) repeating step (c) one or more times to increase the purity of paclitaxel or docetaxel; (e) dissolving the paclitaxel or docetaxel obtained from step (d) in alkanol and then adding water, filtering and drying the solid thus formed, to obtain paclitaxel of increased purity; (f) dissolving the solid obtained from step (e) in alkyl ketone, filtering, followed by adding alkane to the filtrate, filtering and drying the solid thus formed to obtain pure paclitaxel or pure

Abstract: A process for preparing propylene oxide comprises at least the following steps: (a) propene is reacted with a hydroperoxide in a solvent in the presence of a zeolite catalyst to give a mixture (M0), where the mixture (M0) comprises propylene oxide, solvent, unreacted propene, unreacted hydroperoxide and oxygen, (b) the propylene oxide is separated from the mixture (M0) so as to give a mixture (M1) which comprises unreacted propene and oxygen, (c) the mixture (M1) is brought into contact with a liquid medium comprising at least a solvent to give the mixtures (M2) and (M3), where the mixture (M3) comprises part of the unreacted propene and oxygen and the mixture (M2) comprises solvent and residual propene, and ?the mixture (M3) which has been separated off and comprises unreacted propene and oxygen has a ratio of oxygen to propene such that the mixture (M3) is not ignitable, and ?the mixture (M2) is fed to at least one reaction of propene with hydroperoxide.

Abstract: This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions containing such compounds and their use as anti-proliferative agents, especially tumour growth inhibitors and anti-cancer agents, antibiotics and/or antiviral agents.

Abstract: The present invention relates to specific photochromic heterocyclically annellated indenochromene derivatives and the use thereof in plastics of all types, particularly for ophthalmic applications.

Abstract: An improved method for the isolation of taxanes of high purity from the crude extract of naturally occurring Taxus canadensis which comprises the steps of: a) filtering the crude extract by liquid column chromatography; b) enriching the taxanes obtained from step a) by precipitation and crystallization; and c) dissolving the taxanes extract in a polar organic solvent mixture comprising an alcohol and a non-alcohol solvent, which solution is then subjected to further separation by liquid column chromatography, and isolating substantially pure paclitaxel from cephalomannine; and all solvent mixtures used may be collected, purified and recycled without separation.

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

Abstract: A process for the continuous epoxidation of propene with hydrogen peroxide in the presence of a titanium silicalite catalyst and a methanol solvent, wherein the catalyst is periodically regenerated by washing with a methanol solvent at a temperature of at least 100° C. and the epoxidation reaction is carried out for periods of more than 300 h between two regeneration steps.

Abstract: In a process for preparing an ester of an unsaturated carboxylic acid by reacting an ester of the unsaturated carboxylic acid and a C1-C4-alkanol with an alcohol R3OH, where R3 is a C4-C20-alkyl radical, a C5-C7-cycloalkyl radical, a phenyl-C1-C4-alkyl radical or a C2-C12-alkyl radical substituted by at least one NR5R5 group or by from 1 to 3 hydroxyl groups or C1-C4-alkoxyl groups or interrupted by one or more oxygen atoms, where the radicals R5 are, independently of one another, C1-C6-alkyl or together with the nitrogen atom form a 5- to 7-membered heterocyclic ring which may contain a further nitrogen or oxygen atom, in the presence of a transesterification catalyst, the transesterification catalyst used is at least one metal alkanolate containing at least one OR1 group, where R1 is a 2,2,6,6-tetraalkyl-1-oxylpiperidin-4-yl radical.

Abstract: Taxane derivatives having a 3? butenyl substituted C13 side chain.

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