Abstract: The selectivity of an olefin epoxidation process catalyzed by a titanium-containing zeolite is improved by performing the epoxidation in the presence of a non-ionic tertiary amine or tertiary amine oxide additive. For example, when hydrogen peroxide is reacted with propylene in the presence of TS-1 titanium silicalite to form propylene oxide, non-selective ring-opening reactions of the propylene oxide are suppressed when low concentrations of 2,6-lutidine or other substituted pyridines are added to the hydrogen peroxide feed.

Abstract: The present invention provides novel haloenol lactones that are effective as active site inhibitors of cholesterol esterase. By inhibiting cholesterol esterase the inhibitors of the present invention provide a new approach to the treatment of hypercholesterolemia through limiting the bioavailability of dietary cholesterol.

Abstract: A process and catalyst for the direct oxidation of an olefin having three or more carbon atoms, such as propylene, by oxygen to the corresponding olefin oxide, such as propylene oxide. The process involves contacting the olefin with oxygen under reaction conditions in the presence of hydrogen and in the presence of a catalyst. The catalyst comprises gold on a titanosilicate, preferably a microporous or mesoporous titanosilicate, such as, TS-1, TS-2, Ti-beta, Ti-ZSM-48, or Ti-MCM-41. Selectivity to the olefin oxide is high at good conversions of the olefin. The catalyst is readily regenerated, and the time between catalyst regenerations is long.

Abstract: Taxane derivatives having alternative C2 substituents.

Abstract: The present invention relates to an improved process for the production of important taxol analogues 10-deacetyl taxol A,B and C of the formula (2) ##STR1## R=C.sub.6 H.sub.5 (10 deacetyl taxol A) =CH.sub.3 C.dbd.CHCH.sub.3 (10-deacetyl taxol B)=C.sub.5 H.sub.11 (10-deacetyl taxol C)where R represent C.sub.6 H.sub.5 (10-deacetyl taxol A) or, CH.sub.3 C.dbd.CHCH.sub.3 (10-deacetyl taxol B) or, C.sub.5 H.sub.11 (10-deacetyl taxol C) which comprises (a) dissolving the taxol analogues 7-xylosyl-10-deacetyl taxol A,B,C of the formula (1) ##STR2## R=C.sub.6 H.sub.5 (10 deacetyl taxol A) =CH.sub.3 C.dbd.CHCH.sub.3 (10-deacetyl taxol B)=C.sub.5 H.sub.11 (10-deacetyl taxol C)where R represents C.sub.6 H.sub.5 (taxol analogue A or xyloside A), or CH.sub.3 C.dbd.CHCH.sub.3 (taxol analogue B or xyloside B) or C.sub.5 H.sub.11 (taxol analogue C or xyloside C) in a polar solvent (b) reacting the resultant solution with periodate for 20-40 hours at 20-40.degree. C.

Abstract: The present invention provides an efficient route to the C-13 side chain of the anti-cancer drug paclitaxel (TAXOL) and its analogs. The process includes the resolution of racemic erythro 2-hydroxy-3-amino-3-phenylpropionamide by diastereomeric crystallization and its conversion via various intermediates to the threo-ethylester and threo-methylester isomers.

Abstract: Borneol derivatives of formula I ##STR1## in which R.sup.1 to R.sup.5 and X.sup.1 to X.sup.2 are defined in the specification, and the method of making the same.

Abstract: Substituted tetrahydrofuran analogs of F-series prostaglandins and methods of their use in treating glaucoma and ocular hypertension are disclosed.

Abstract: An efficent synthesis of furan sulfonamide compounds of formula ##STR1## comprising reacting a compound of formula 11 with a Grignard reagent in a reaction inert solvent, wherein R' is (C.sub.1 -C.sub.6)alkyl. The compound of formula II is prepared by reacting a compound of formula III with a compound of formula IV wherein R' is (C.sub.1 -C.sub.6)alkyl with a chorinating reagent and an acid scaverger in an inert solvent. The invention also includes a novel compound of the formula ##STR2## wherein R' is (C.sub.1 -C.sub.6)alkyl and Q is halo, hydroxy or amino.

Abstract: Process for the preparation of 4-acetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1,7.beta., 10.beta.-trihydroxy-9-oxo-tax-11-en-13.alpha.-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate trihydrate, characterized in that the 4-acetoxy-2.alpha.-benzoyloxy-5.beta.,20-epoxy-1,7.beta.,10.beta.-trihydro xy-9-oxo-tax-11-en-13.alpha.-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate is crystallized from a mixture of water and an aliphatic alcohol containing 1 to 3 carbon atoms, and then the product obtained is dried under defined conditions of temperature, pressure and humidity.

Abstract: The invention provides various derivatives of arglabin, a sesquiterpene lactone isolated from Artemisia glabella. These compounds are effective for suppressing tumor growth in mammals. A method of suppressing tumor growth in humans is also described.

Abstract: Process for synthesizing paclitaxel by treating baccatin III with a strong base in a solvent, adding an electrophile to the solution to form a 7-O-protected baccatin III derivative, reacting the 7-O-protected baccatin III derivative with a protected paclitaxel sidechain in a solvent such that the protected paclitaxel sidechain is coupled to the 13-hydroxyl of the 7-O-protected baccatin III, and subsequently deprotecting the protected paclitaxel sidechain and the 7-O protecting group to form paclitaxel, and intermediates used therein.

Abstract: Taxane derivatives having an alkoxy, alkenoxy or aryloxy substituted C13 side chain.

Abstract: A process for recovering 3,4-epoxy-1-butene from a vapor phase catalytic oxidation reactor effluent where 1,3-butadiene is reacted with oxygen over a silver catalyst, the process includes the steps of contacting the reactor effluent with an absorbent in an absorber and vaporizing in the absorber an effective amount of a non-reactive coolant to cool the absorber to a temperature of less than about 40.degree. C. and a pressure of less than about 4 bar. Advantageously, the vaporization of the non-reactive coolant proximate to the absorber allows the absorber to be operated at lower temperatures and pressures than heretofore possible and provides a further advantage of allowing higher O.sub.2 concentrations in the feed to the epoxidation reactor.

Abstract: A process and apparatus for manufacture of organic products, particularly chemical intermediates, by oxidation of organic feedstocks. A membrane unit containing a membrane selectively permeable to the organic over argon is used to recover the feedstock from the argon purge stream.

Abstract: Taxane derivatives having alternative C9 substituents.

Abstract: The present invention is directed to a process for the selective epoxidation of non-allylic olefins. The process includes the step of contacting a gas mixture comprising a non-allylic olefin, oxygen, and a fluorinated hydrocarbon with a silver epoxidation catalyst at conditions effective to epoxidize the non-allylic olefin. The fluorinated hydrocarbon has a C--F bond dissociation energy of 110 kcal/mole or greater, and sufficiently non-acidic C--H bonds, if present, so as to avoid abstraction of HF from the fluorinated hydrocarbon under reaction conditions.

Abstract: An oxidation catalyst based on titanium silicalites or vanadium silicalites having a zeolite structure and containing from 0.01 to 30% by weight of one or more noble metals selected from the group consisting of ruthenium, rhodium, palladium, osmium, iridium, platinum, rhenium, gold and silver has been molded by a compacting shaping process.This oxidation catalyst is used for the preparation of epoxides, in particular propylene oxide, from olefins, hydrogen and oxygen.

Abstract: The selectivity of an olefin epoxidation catalyzed by a noble metal-modified titanium or vanadium zeolite is greatly enhanced by the addition of a nitrogen compound to the reaction mixture. The epoxidation utilizes hydrogen and oxygen in addition to the olefin.