Abstract: A group of 2-amino-3-aroyl-benzo[.beta.]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo[.beta.]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6 -hydroxy-2-(4-hydroxyphenyl )-3-[4-(2 -piperidinoethoxy)benzoyl]benzo[.beta.]thiophene.

Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed. The analogs have the general formula: ##STR1## wherein NH--R is a selected aryl amine, dialkylaminoalkyleneamino, or dialkylaminoanilino group.

Abstract: The present invention provides two 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 analogs to taxol. Both the intermediates and analogs to taxol may prove to be valuable anticancer agents.

Abstract: This invention concerns a process for the preparation of polyfluorooxetanes by the reaction of fluoroketones or fluoroepoxides with haloethylenes in the presence of a Lewis acid catalyst. Polyfluorooxetanes are useful as solvents and plasticizers having high thermal stability.

Abstract: A short route to the total synthesis of the core skeleton of the taxol ring system is described. The same sequence of transformations can be carried out to make the 7-hydroxy series, and connect the additional carbon atoms required for the A-ring. The number of steps to the taxane skeleton is 13, making it the shortest route from readily available inexpensive starting materials.

Abstract: A lactone is prepared by catalytically hydrogenating a dicarboxylic acid having 3 to 10 carbon atoms or a functional derivative thereof in the presence of a catalyst comprising a metal selected from the elements of group VIII of the periodic table or a combination of said metal with an element selected from the elements of groups IVa, VIb and VIIb of the peridic table, and further in the co-presence of an alkali metal salt or an alkali metal hydroxide.

Abstract: Compound (1), isolated from a marine dinoflagellate, is a novel macrolide which has potent in vitro cytotoxicity against human colon carcinoma cell line HCT116 (IC.sub.50 =1.6 nM) and a multiple drug resistant subline. In addition, this compound has good in vivo antitumor activity against a P388 mouse leukemia (150% T/C).

Abstract: Taxane derivatives having a 3' pyridyl substituted C13 side chain.

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: This invention provides microporous alkali metal bicarbonate, which can contain an absorbed gaseous, liquid or solid phase as an encapsulated ingredient. A present invention microporous bicarbonate composition has utility as a lightweight deodorant ingredient in a cosmetic stick or roll-on product. This permits the solid organic matrix and dispersed deodorant particle phases to have densities which are sufficiently matched to prevent setting of the dispersed particles during manufacture, and to provide a cosmetic stick or roll-on product with dimensional stability.

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 catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,R.sup.3 is hydrogen, lower alkyl, optionally substituted benzyl, --CO--R.sup.4, --COOR.sup.4 or --CONR.sub.2.sup.4, andR.sup.4 is lower alkyl or aryl,comprising asymmetrically hydrogenating a compound of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the above significance, in the presence of a complex of an optically active, preferably atropisomeric, diphospine ligand with a metal of Group VIII.

Abstract: This invention relates to derivatives of Wortmannin and particularly to 11,17 substituted derivatives of Wortmannin. The invention also relates to a method of using these compounds as PI-3-kinase inhibitors and as anti-tumor agents.

Abstract: R.sup.g is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Further provided by this invention are pharmaceutical formulations and intermediates for the the preparation of deoxy taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

Abstract: The invention features phototherapeutic compositions comprising Type 1, Type 2, or Type 3 psoralens and methods of using such compounds for treatment of proliferative diseases of skin, blood and bone marrow.

Abstract: A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial cancer, endometriosis, mastopathy, etc.This compound is characterized in that the 2-position (the substituent R.sup.2) of the benzothiophene nucleus is substituted by a halogen atom; a lower alkyl group; or a cycloalkyl or cycloalkenyl group optionally substituted by a lower alkyl group, a hydroxyl group, acyloxy group or an oxo group.

Abstract: The natural product cephalomannine can be converted to the important anticancer natural product taxol by a simple process involving the steps of dihydroxylation to give cephalomannine-diols, diol cleavage, benzoylation at the 2'-position and reaction with a 1,2-diamine. The same process when applied to mixtures of taxol and cephalomannine makes it possible to separate taxol from cephalomannine-diols by simple flash-chromatography after the dihydroxylation step. If the benzoylation step is avoided in the above sequence of conversions, the process leads to the free amine (N-debenzoyltaxol). In addition, the selection of an acylating reagent other than that with the benzoyl group for acylation of the free amine (N-debenzoyltaxol), allows the preparation of taxol analogs with other N-acyl substituents.

Abstract: A compound or prodrug thereof having the formula ##STR1## wherein --OR.sup.1 comprises the C-13 side-chain of taxol and Z is selected from the group consisting of --CHO, --CH.sub.2 OH, --CH.sub.2 OR', --CH.sub.2 NR'R", --CH.dbd.NR', --CH.dbd.NOR', --CH.dbd.NNR.dbd.R", --CH(OH)SO.sub.3 Na, --CH.sub.2 OPO.sub.3.sup..dbd., --CH.sub.2 OSO.sub.3.sup..dbd., --CN and a radical of the formula ##STR2## where X and Y are independently selected from --O--, --S--, and --N(R')--, as well as a method for preparing the compounds of the invention, a method of their use for the inhibition of tumors and pharmaceutical compositions containing the same.

Abstract: A group of 2-amino-3-aroyl-benzo[.beta.]thiophenes are prepared by treating an aldehyde with an anion of dimethylamino thioformamide, cyclizing the .alpha.-hydroxy thioamide, and subsequently acylating the benzo[.beta.]thiophene to yield the 2-amino-3-aryl derivative. These compounds may be treated with suitable phenyl Grignard reagents, and after deprotection, yield 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyl]benzo[.beta .]thiophene.

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