Abstract: A method for the synthesis of bis-tetrahydrofranyl Annonaceous acetogenins, including the natural products and analogs thereof, is provided which proceeds by the Pd-mediated coupling of a bis-tetrahydrofuranyl-subunit comprising a terminal alkyne, with a (C4)-hydroxybutenolide subunit comprising a terminal vinyl iodide, followed by selective reduction of the resulting enyne.

Abstract: Propylene is separated from the methanol present as a solvent in a crude olefin epoxidation product by means of an extractive distillation wherein a relatively heavy polar solvent having hydroxy groups such as water or propylene glycol is used as the extractive solvent. The method is also useful for removing water and impurities such as acetaldehyde from the propylene oxide.

Abstract: An olefin epoxidation process is operated using a plurality of reactor vessels, each containing a fixed bed of a heterogeneous catalyst such as titania-on-silica. The reactor vessels are connected in series whereby a feedstream comprised of olefin and an active oxygen species is passed through said series of reactor vessels in contact with the heterogeneous catalyst to accomplish conversion of the olefin to the corresponding epoxide. As the activity of the catalyst in an individual reactor vessel falls to an undesirably low level, said reactor vessel is taken out of service and a replacement reactor vessel containing fresh or regenerated catalyst introduced. The replacement reactor vessel may, in alternative embodiments of the process, be the first or the last reactor vessel in said series. For example, the feedstream may first be contacted with either the most active or the least active charge of catalyst within the series of reactor vessels.

Abstract: Disclosed are compounds of Formula I: ##STR1## wherein R.sup.1 through R.sup.6 are defined herein. Also disclosed are pharmaceutical compositions and methods of using these compositions for treating retroviral infections. Finally, a stereoselective method for synthesizing compounds of Formula I is described.

Abstract: New taxoids of general formula (I): ##STR1## their preparation and pharmaceutical compositions containing them, and the new products of general formula (I) in which Z represents a radical of general formula (II): ##STR2## display noteworthy antitumour and antileukaemic properties.

Abstract: A new class of stable dioxetanes bears a polycyclic stabilizing group and aryloxy moiety, the oxygen atom of which is provided with a protective group which can be removed by an enzymatic or chemical trigger admixed with the dioxetane. The polycyclic stabilizing group is preferably spiroadamantane. The group further bears an alkoxy, aryloxy, aralkyloxy or cycloalkyloxy moiety which is partially or completely substituted with halogens, particularly fluorine and chlorine. Proper selection of electron active groups on the stabilizing moiety, the aryl group and the OR group yields enhanced enzyme kinetics, superior light intensity and excellent detection sensitivity in various assays.

Abstract: An optically-purified enantiomer of the lactone 4-hydroxy-2-oxabicyclo-?3.3.0!oct-7-en-3-one or an acylate thereof can be obtained by biotransformation. It is a useful synthon in the preparation of an enantiomer of 3-hydroxymethyl-2-hydroxycyclopentene that can be used to prepare carbocyclic nucleosides as a desired enantiomer.

Abstract: This invention relates to compounds of the formula (I), preparation thereof, and pharmaceutical compositions containing them: ##STR1## wherein: R.sub.a is hydrogen, hydroxyl, alkoxy, acyloxy, or an alkoxyacetoxy radical; R.sub.b is hydrogen; or R.sub.a and R.sub.b, together with the carbon atom to which they are attached, form a ketone function; Z represents a hydrogen atom or a radical of formula (II): ##STR2## in which: R.sub.1 represents an optionally substituted benzoyl, thenoyl, furoyl, or R.sub.2 --O--CO-- radical where R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, or an optionally substituted phenyl or heterocyclic radical; R.sub.3 is an aromatic heterocyclic, alkyl, alkenyl, alkynyl, cycloalkyl, or a phenyl or naphthyl radical; R.sub.4 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, aryl, or heterocyclic radical; and R.sup.5 is an optionally substituted cycloalkenyl, alkyl, alkenyl, alkynyl, or cycloalkyl radical.

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

Abstract: Provided are antineoplastic derivatives by a process of selective halogenation of side chains of unsaturated taxanes; more particularly, the process involves the use of halogens, particularly bromine, which is easily added to the side chain double bond of cephalomannine, leaving paclitaxel unchanged, and wherein diastereomeric mixtures of 2", 3"-dibromocephalomannine display high activity against: Leukemia cell line HL-60 (TB); Non-Small Cell Lung Cancer line NCI-H522; Colon Cancer cell lines COLO 205 and HT 29; CNS Cancer cell lines SF-539 and SNB-75; Ovarian Cancer Cell line OVCAR-3; Renal Cancer cell line RXF-393; and Breast Cancer cell lines MCF7, MDA-MB-231/ATCC, HS 578T, MDA-MB-435 and MDA-N.

Abstract: A reactor and process is for the production of oxirane compounds by reaction of an olefin such as propylene with an organic hydroperoxide using a solid contact catalyst, characterized by the following features:(1) the reactor is divided into a series of separate zones, each zone containing a bed of solid epoxidation catalyst;(2) conditions are maintained so as to provide the liquid phase without substantial vapor formation throughout the entire reactor;(3) cold reactor feed is provided which is preheated to reaction temperature by separate indirect heat exchange with reaction liquid from various of the separate reactor zones;(4) reaction liquid from the last of the series of reaction zones is reduced in pressure to form a gas-liquid mixture at a lower temperature, and this gas liquid mixture is heated by indirect heat exchange with the reaction liquid from at least one of the separate reactor zones.

Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;R.sub.1 is selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;(n) is an integer from 1 to about 12; andR.sub.2 is a polyalkylene oxide.In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.

Abstract: Provided are antineoplastic derivatives by a process of selective halogenation of side chains of unsaturated taxanes; more particularly, the process involves the use of halogens, particularly bromine, which is easily added to the side chain double bond of cephalomannine, leaving paclitaxel unchanged, and wherein diastereomeric mixtures of 2", 3"-dibromocephalomannine display high activity against: Leukemia cell line HL-60 (TB); Non-Small Cell Lung Cancer line NCI-H522; Colon Cancer cell lines COLO 205 and HT 29; CNS Cancer cell lines SF-539 and SNB-75; Ovarian Cancer Cell line OVCAR-3; Renal Cancer cell line RXF-393; and Breast Cancer cell lines MCF7, MDA-MB-231/ATCC, HS 578T, MDA-MB-435 and MDA-N.

Abstract: Halogen magnesium aluminum hydridohalides of the general formula?Mg.sub.2 X.sub.3 (ether).sub.y !.sup.+ ?AlH.sub.4-n X.sub.n !.sup.-wherein X is chlorine, bromine or iodine, y is a number from 0 to 6, n is a number from 1 to 3 and ether is an aliphatic or cylcoaliphatic ether with 2 to 30 carbon atoms, with the exception of t-butyl ether, with a dipole moment>0.5 Debye and a melting point of<0.degree. C. are prepared. The invention furthermore relates to a method for the synthesis of these compounds and to a method of reducing functional organic compounds utilizing the inventive compounds.

Abstract: The present invention comprises 6,8-difluoro-7-hydroxycoumarins and derivatives of 6,8-difluoro-7-hydroxycoumarins, including reactive dyes, dye-conjugates and enzyme substrates. These fluorine-substituted fluorescent dyes typically possess greater photostability and lower pH sensitivity in the physiological pH range than their nonfluorinated analogs, exhibit less fluorescence quenching when conjugated to a substance, possess absorption and emission spectra that closely match those of their nonfluorinated analogs, and also exhibit higher quantum yields than their nonfluorinated analogs.

Abstract: Taxane-based compositions of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of aryls, substituted aryls, aralkyls, substituted aralkyls, alkyls and substituted alkyls;R.sub.2 is an aryl or substituted aryl, preferably phenyl;R.sub.3 is H, a C.sub.1-10 alkoxy, SiEt.sub.3 or ##STR2## Y is O or S; (n) is zero or a positive integer;X is oxygen, S, SO.sub.2 or NL, where L is selected from the group consisting of H, C.sub.1-8 alkyls, aryls and aralkyls;R.sub.4 is H or an aroyl of the formula: ##STR3## wherein Ar is an aromatic, substituted aromatic or heteroaromatic group; R.sub.5 is H, CH.sub.3 CO or a substituted acetic acid derivative;Z is H or OR.sub.6 where R.sub.6 is selected from the group consisting of H, C.sub.1-8 alkyls, C.sub.1-8 substituted alkyls, C.sub.1-8 aralkyls, substituted aryls, aralkyls, substituted aralkyls, C.sub.1-10 alkoxy, SiEt.sub.3, ##STR4## P is O or OH; R.sub.8 is one of H, S(CH.sub.3).sub.3, Si(C.sub.2 H.sub.5).sub.3, CH.sub.

Abstract: This invention provides 7-deoxy-.DELTA..sup.12,13 -iso-taxol of formula (I) which are useful for the treatment of the same cancers for which taxol has been shown active.

Abstract: Alkaline sensitive protaxol is water soluble and is hydrolyzed at physiological (alkaline) pH to render the native taxol structure and the native taxol activity. Protaxol compositions include 2'- and/or 7-O-ester derivatives of taxol and/or 2'- and/or 7-O-carbonate derivatives taxol. Protaxol has a formula as follows: ##STR1## wherein R.sup.1 and R.sup.2 are each H or a radical selected from the group consisting of --CO--(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --COZ and --COO--(CH.sub.2).sub.o --Y--Ar, and wherein m, n, and o are each an integer of 1 to 3; X is 0, S, NH, SO, or SO.sub.2 ; Y is S, SO or SO.sub.2 ; Ar is phenyl or substituted phenyl wherein the substituent is halo, amino, nitro or N,N-dialkylamino having 1 to 4 carbons in each of the alkyl groups; and Z is OH, OR.sup.3, SR.sup.3 or NR.sup.4 R.sup.5 wherein R.sup.3 is alkyl containing 1 to 4 carbons and R.sup.4 and R.sup.

Abstract: The present invention is directed to novel taxoids possessing strong reversing activities for drug-resistance associated with anti-cancer agents, the preparation of these reversal agents and pharmaceutical compositions thereof. The new taxoids of the present invention have the formula (I).

Abstract: Provided are novel paclitaxel analogues, namely selectively brominated stereospecific derivatives of cephalomannine and 7-epi-cephalomannine having in vivo and in vitro paclitaxel-like antitumor efficacy, methods of preparation therefor and methods for treating tumors with these compounds.