Abstract: The present invention relates to a proces for manufacturing L-(-)-carnitine from D-(+)-carnitine or a derivative thereof. D-(+)-carnitine is esterified in order to protect the carboxyl group and subsequently converted to an acyl derivative. The acyl derivative is then converted to a lactone of L-(-)-carnitine. Finally, the lactone is reopened to obtain L-(-)-carnitine.

Abstract: The present invention relates to a process for producing dl-tocopherols and intermediates for the production. dl-Tocopherols obtained by the present invention are useful compounds that are used as food additives, feed and medicaments.

Abstract: A bisphenol derivative represented by the following formula and a manufacturing method thereof are disclosed: ##STR1## where R is a lower alkyl group, tetrahydropyranyl, methoxymethyl or trialkylsilyl group, and the benzene rings in the formula may be substituted by a lower alkyl group.

Abstract: A two-step process for converting ginkgolide C into ginkgolide B is disclosed. In the first step, ginkgolide C is reacted with a sulfonic anhydride to obtain a C-7 sulfonate of ginkgolide C. In the second step, the C-7 sulfonate of ginkgolide C is reacted with a borohydride, and this reaction eliminates the C-7 radical of the C-7 sulfonate of ginkgolide C, thus producing ginkgolide B.

Abstract: The present invention provides three basic routes for the total synthesis of taxol having the structure: ##STR1## The present invention also provides the intermediates produced in the above processes, processes for synthesizing these intermediates as well as analogues of taxol and nortaxol.

Abstract: Anomeric 2,2-difluororibosyl azide and amine intermediates which are useful for the preparation of 2'-deoxynucleosides, and processes thereto, are provided. Processes for preparing 2'-deoxynucleosides also are provided.

Abstract: A method for the synthesis of bis-tetrahydrofuranyl 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: The invention relates to a process for preparing taxoids of formula I herein that includes the steps of esterifying a baccatin III derivative of the formula VI herein, acylating the compound obtained, and optionally removing a protecting group to give the desired taxoid product.

Abstract: Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C2 substituent other than benzoate and/or a C4 substituent other than acetate in which the C2 benzoate substituent and/or the C4 acetate substituent of a derivative of baccatin III or 10-desacetyl baccatin III is/are selectively reduced to the corresponding hydroxy group(s) and converted to R.sub.7 COO-- and/or R.sub.8 COO--, respectively, wherein R.sub.7 and R.sub.8 are independently H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.2 alkenyl, C.sub.2 -C.sub.6 alkynyl, moncyclic aryl, or monocyclic heteroaryl.

Abstract: A method for reduction of an allyl alcohol-type compound, specific to its allylic hydroxyl group, being carried out without any side reactions such as reduction of other portions of the compound or allylic rearrangement, which comprises treating the compound with trialkylsilane in the presence of AlX.sub.3, wherein X refers to a halogen atom.

Abstract: The invention relates to a process for preparing taxoids of formula I herein that includes comprising the steps of esterifying a baccatin III derivative of the formula VI herein, treating the compound obtained in acidic medium, and optionally removing a protecting group to give the desired taxoid product.

Abstract: New Baccatin III derivatives are disclosed for use in making taxoid compounds having formula (I) illustrated herein that exhibit antitumor activity.

Abstract: A process for the preparation of Iopamidol and 5-amino-2,2-dialkyl-1,3-dioxanes of formula ##STR1## wherein R and R.sub.1 are the same or different and represent a straight or branched C.sub.1 and C.sub.2 alkyl group or together with the carbon atom to which they are bonded, form a C.sub.5 -C.sub.6 cycloaliphatic ring; comprising the transformation of a 2,2-dialkyl-1,3-dioxane-5-carboxylic acid ester of formula ##STR2## wherein R.sub.2 represents a straight or branched C.sub.1 -C.sub.2 alkyl group, a phenyl optionally substituted by nitro groups or a benzyl; by treatment with ammonia into the corresponding amides and the subsequent rearrangement of the latter into the compounds of formula I, by treatment with a hypohalogenite. The resultant ketals may be used as is, or be converted to 2-amino-1,3-propanediol, and reacted with 5-amino-2,4,6-triiodo-isophthalic acid dichloride or, alternatively,L-5-(2-acetoxy-propionylamino)-2,4,6-triido-isophthalic acid dichloride, to produce Iopamidol.

Abstract: This invention provides a taxane derivative of the formula: ##STR1## wherein a hydrophobic organic moiety is attached to a taxane. R and R.sup.1 is each indepently H or a hydrophobic organic moiety, as long as at least one of R and R.sup.1 is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

Abstract: This invention relates to process for the preparation of a taxane derivative of general formula (I): ##STR1## and use of the product obtained for the preparation of taxane derivatives of general formula (II): ##STR2## In the general formula (I), R.sub.1 is an acetyl radical or a protective grouping G.sub.1 is a protective grouping and R is a t-butoxy or phenyl radical. In the general formula (II), R is a t-butoxy or phenyl radical and R'.sub.1 is a hydrogen atom or an acetyl radical.

Abstract: Psoralen compound compositions are synthesized which have substitutions on the 4, 4', 5', and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.

Abstract: The invention relates to a process for preparing taxoids of formula I herein that includes the steps of esterifying a baccatin III derivative of the formula VI herein, treating the compound obtained in acidic medium, and optionally removing a protecting group to give the desired taxoid product.

Abstract: A compound of the formula ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also provided by the invention are methods of use of the above compounds, and processes for the preparation thereof.

Abstract: The present invention relates to an epoxycyclohexenedione derivative represented by formula (I): ##STR1## wherein R is a straight-chain or branched alkanoyl group having 10 to 25 carbon atoms, a straight-chain alkenoyl group having 10 to 25 carbon atoms, or a group represented by formula (A): ##STR2## wherein n is an integer of 1 to 4; or a pharmaceutically acceptable salt thereof.The compounds exhibit antimicrobial activity and antitumor activity.

Abstract: There are provided methods to control monocotyledenous weed species in the presence of crops and particularly in the presence of cereal crops. Also provided are 4-(2,6-disubstituted-phenoxy)coumarin derivatives useful as herbicidal agents and methods to prepare same.