Abstract: Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: ##STR1## wherein R.sub.1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R.sub.2 is hydrogen, ethoxyethyl, 2,2,2-trichloroethoxymethyl or other hydroxyl protecting group; and R.sub.3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; the contacting of said alcohol and oxazinone being carried out in the presence of a sufficient amount of an activating agent under effective conditions to cause the oxazinone to react with the alcohol to form a .beta.-amido ester which is suitable for use as an intermediate in the synthesis of taxol.

Abstract: A polyamic acid or polyimide having 2,5-distyrylpyrazine units in the main chain thereof.

Abstract: Compounds of Formula 1, and of Formula 2, ##STR1## in which R.sub.1 is H or alkyl of 1 to 20 carbon, CO--R.sub.1 * CO--O--R.sub.1 * CO--NH--R.sub.1 * or PO(OR.sub.1 *).sub.2 or PO(OR.sub.1 *)R.sub.1 * where R.sub.1 * independently is alkyl of 1 to 20 carbons, phenyl, or substituted phenyl; X is long chain alkyl having at least 5 carbon atoms, long chain alkyl of at least 5 carbons substituted with an aryl group, or long chain alkyl of at least 5 carbons substituted with a substituted aryl group; Y is COOH, COOR.sub.2, CONH.sub.2, CONHR.sub.2, CON(R.sub.2).sub.2, CHO, COR.sub.2 ; COCF.sub.3, COCHF.sub.2, CH.dbd.NR.sub.2, CR.sub.2 .dbd.N--R.sub.2, CH.dbd.N--NHR.sub.2, CH.dbd.N--N(R.sub.2).sub.2, CH.dbd.NOH, CR.sub.2 .dbd.N--OH, CH.dbd.NOR.sub.2, CR.sub.2 .dbd.NOR.sub.2, CH.sub.2 OH, CHR.sub.2 OH, C(R.sub.2).sub.2 OH, CH.sub.2 OR.sub.2 * CHR.sub.2 OR.sub.2 * C(R.sub.2).sub.2 OR.sub.2 * SO.sub.2 R.sub.2, PO(OR.sub.3).sub.2, and PS(OR.sub.3).sub.2, where R.sub.

Abstract: 2'-Deoxy-3',5'-diacyl-5-fluorouridines useful as antitumor medicines or intermediates thereof are easily and efficiently obtained by first fluorinating 2'-deoxyuridine in aqueous solution with fluorine gas to thereby form 2'-deoxy-5,6-dihydro-5-fluoro-6-hydroxyuridine, which is a novel compound, and reacting this compound with a carboxylic acid anhydride or halide R--CO--X, where R is an aliphatic group having not more than 20 carbon atoms or a substituted or unsubstituted phenyl group, and X is an acyloxy group RCO.sub.2 or a halogen atom. In the initial fluorination reaction the aqueous solution may contain a carbonate (or a hydrogen carbonate) or a lower fatty acid or its salt to capture hydrogen fluoride formed by the reaction. The next acylating reaction can be promoted by carrying out the reaction in the presence of an organic base such as pyridine.

Abstract: The reaction of N-substituted piperazines with carboxylic acids or their active derivatives such as lower-alkyl esters or the acid chlorides, leads to the formation of new piperazine carboxamides of general structural formula I: ##STR1## These compounds and the physiologically acceptable salts thereof are useful as analgesics and antiinflammatory agents.

Abstract: 2-(Heterocyclylalkyl)imidazopyridines having antihistaminic properties, compositions containing these compounds as active ingredient and novel 2-(Heterocyclylalkyl)imidazopyridines.

Abstract: A process for the preparation of 2-amino-4-fluoropyrimidine derivatives of the general formula I ##STR1## (R.sup.1 hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or benzyl, it being possible for the aromatic rings to be substituted, and R.sup.2 one of the R.sup.1 radicals with the exception of hydrogen) by reaction of 2,4,6-trifluoropyrimidine in an aprotic polar organic solvent with an amine of the formula III to give the 2-aminodifluoropyrimidine derivative IVa mixed with the 4-aminodifluoropyrimidine derivative IVb, separation of IVa out of the resulting reaction mixture and subsequent reaction of IVa with an alcohol in the presence of a base at from 0.degree. to 180.degree. C. to give the 2-amino-4-fluoropyrimidine derivative I, by carrying out the reaction of 2,4,6,-trifluoropyrimidine II with the amine III at from -80.degree. C. to -15.degree. C.

Abstract: Novel diacylglycerophosphoric acid esters include a hydrophobic diacyl glycerol portion to provide water insolubility and a head group which forms a chromophore or a chromophore precursor when the head group is enzymatically released and are chromogenic substrates useful to assay for enzymes catalyzing the cleavage of phosphate ester or phosphoanhydride bonds adjacent or opposite to the phosphatidic acid region of a phospholipid molecule.

Abstract: Improved method for the manufacture of plant regulant pyridazine-4-one carboxylic acids, which comprises the step of decarboxylating a 4-oxo-3, 5-pyridazine dicarboxylic acid to give a 4-oxo-5-pyridazine carboxylic acid by treatment with 95-100% sulphuric acid at 160.degree.-180.degree. C. using a reactant; acid weight ratio of about 1:4 to 1:10.

Abstract: A process for the production of trimellitic anhydride with improved color properties disclosed. This process comprises treating trimellitic anhydride with an activated silicon compound followed by fractionation and at temperatures of about 200.degree. to about 300.degree. C. and a decreasing pressure of about 1 to about 25 mm Hg. Trimellitic anhydride is used in the manufacture of polyesters and polyamides-imides.

Abstract: This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by alkyl or halogen;R.sup.2 is selected from alkyl; haloalkyl; alkoxy; alkylamino; dialkylamino; halogen; cycloalkyl optionally substituted by halogen or alkyl; and phenyl optionally substituted by alkyl, haloalkyl, halogen or alkoxy;R.sup.3 is selected from hydrogen and halogen;R.sup.4 is the residue of an alcohol of formula R.sup.4 -OH which forms an insecticidal ester when combined with chrysanthemic acid, permethrin acid or cyhalothrin acid; andX is selected from oxygen and sulphur.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted alicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: A multistep process is disclosed for preparing azetidinone intermediates used in the making penems and carbapenems wherein intermediates containing ##STR1## R' is independently hydrogen or 1, 2 or 3 of lower alkyl or lower alkoxy, preferably hydrogen, wherein R" is methyl, ethyl, a phenyl or alkyl, preferably ethyl, as a readily removable nitrogen protecting group are made.

Abstract: Disclosed is a compound containing a 2-amino-7-(substituted methyl)-3H,5H-pyrrolo[3,2-d]pyrimidin-4-one wherein substituted methyl is --CH.sub.2 --R wherein R is an optionally substituted heteroalicyclic group, a pharmaceutical composition containing the compound, and a method for the selective suppression of mammalian T-cell function without diminished effect on humoral immunity which involves administering the composition to a mammal.

Abstract: A method of regioselectively and stereoselectively synthesizing forskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-on e) from 9-deoxyforskolin (8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one) with a good yield is described. In a preferred embodiment, it comprises an enol ether formation from 8,13-epoxy-1.alpha.,6.beta.,7.beta.-trihydroxylabd-14-en-11-one-6,7-carbon ate, oxidation of the enol ether with a suitable peroxy acid to obtain 11,12-dehydro-8,13-epoxy-11-methoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetr ahydrolabd-14-ene-6,7-carbonate and hydrolysis of the latter under an acidic condition to obtain 8,13-epoxy-1.alpha.,6.beta.,7.beta.,9.alpha.-tetrahydroxylabd-14-en-11-one -6,7-carbonate. As an alternative way of protecting the two hydroxy groups at carbon-6 and carbon-7, they may also be converted to dimethyl acetal during the synthetic sequence. Four compounds produced in the synthetic scheme as intermediates, namely, 9,11-dehydro-8,13-epoxy-11-methoxy-1.

Abstract: A pyrimidinedione derivative compound has a basic backbone in which a phenyl group part and a pyrimidinedione part are linked by a structure comprising an alkyl chain containing at least two nitrogen atoms. The pyrimidinedione derivative is useful for a medical treatment of cardiac arrhythmias.

Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.

Abstract: A di(fluoroalkyl containing group-substituted alkyl) phosphate salt which is useful for a surface active agent, a water- and/or oil-repellent for fiber or paper or an oil resistant agent, can be prepared a process which comprises hydrolyzing a mono-sec.- or tert.-alkyl (di(fluoroalkyl containing group-substituted alkyl) phosphate with a base.

Abstract: New benzo[b][1,8]naphthyridine derivatives of general formula (I) in which R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy or alkylamino radical and R.sub.3 is alkyl, R.sub.4 and R.sub.5 are different and are hydrogen or alkyl, or R.sub.3 is H, alkyl or cycloalkyl and R.sub.4 and R.sub.5 are hydrogen, R.sub.6 is hydrogen or fluorine and n is equal to 1 or 2, their salts, their preparation and the compositions which contain them.

Abstract: The invention relates to novel substituted azacyclohexyl derivatives of formula ##STR1## and salts of thereof in which the structural elements --A.sub.1 -A.sub.2, --A.sub.3 -A.sub.4 -- and --A.sub.5 -A.sub.6 -- are each ethylene or vinylene or the elements --A.sub.1 -A.sub.2 -- and --A.sub.3 -A.sub.4 -- are each ethylene and --A.sub.5 -A.sub.6 -- is vinylene, X is >CR.sub.6 -- or >N-- and R.sub.6 is alkyl or hydrogen, alk is an aliphatic hydrocarbon radical or a bond, R.sub.1 is hydrogen or acyl, R.sub.2 is hydrogen or acetyl, R.sub.3 and R.sub.4 together are a bond or each is hydrogen, R.sub.5 is hydrogen, a cycloaliphatic hydrocarbon radical, aryl or heteroaryl and R.sub.7 is hydrogen or alkyl, with the proviso that when --A.sub.1 -A.sub.2 --, --A.sub.3 -A.sub.4 -- and --A.sub.5 -A.sub.6 -- are each vinylene, X is >N--, R.sub.1 is hydrogen or trialkylacetyl, R.sub.2 is hydrogen or acetyl, R.sub.3 and R.sub.4 together are a bond and alk is methylene, R.sub.