Abstract: A process for producing an unsymmetrical chain carbonic acid ester is described, which comprises reacting a first symmetrical chain carbonic acid ester with a second symmetrical chain carbonic acid ester or a monohydric alcohol in the presence of a catalyst comprising as an active catalyst component an oxide of at least one element selected from the Group IIIB elements of the periodic table.

Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which R.sub.1, R.sub.2 and R.sub.3 independently represent hydrogen, hydroxy, halo, alkyl or alkoxy;ALK.sup.1 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups;Y represents a piperidine ring which is attached through nitrogen to ALK.sup.1 ;R.sub.4 represents hydrogen or a C.sub.1-4 alkyl group; the broken line in --- represents a bond, or is absent and the free valency on Y is taken up by hydrogen and the free valency on CR.sub.4 is taken up by hydrogen or a C.sub.1-4 alkyl group;ALK.sup.2 is absent or represents a C.sub.1-4 alkylene chain optionally substituted by one or more C.sub.1-2 alkyl groups; andR.sub.5 and R.sub.6 independently represent hydrogen, alkyl, phenyl, alkyl (optionally substituted) or R.sub.5 and R.sub.

Abstract: A practical synthesis of the potential chemotherapeutic agent L-azatyrosine is described. The key step involved the alkylation of (R,R)-(-)-pseudoephedrine glycinamide with 5-benzenesulfonyloxy-2-iodomethylpyridine and proceeded in 70-95% yield and 89-95% de. Simultaneous hydrolysis of the auxiliary and the benzenesulfonate protecting group afforded L-azatyrosine of .gtoreq.99% ee in 73% yield on multigram scale (recovery yield of (R,R)-(-)-pseudoephedrine: 90%).

Abstract: Hydroxyquinolone monoazo dyestuffs of the formula I ##STR1## in which D is an organic radical such as one of the disclosed aromatic radicals, and R is substituted or unsubstituted alkyl, benzyl, phenyl, phenoxy, or alkoxy (most preferably C.sub.1 -C.sub.6 -alkyl) are especially well suited to dyeing and printing of hydrophobic materials and other dyeing or printing applications. The dyestuffs are prepared by diazotizing an amine (D--NH.sub.2) and coupling the diazotization product to a hydroxyquinolone compound.

Abstract: A method and system for effecting withdrawal from caffeine dependency is disclosed wherein the system comprises a regiment of dosage units having varying proportions of caffeine and an analgesic. One embodiment utilizes a first dosage unit which has a caffeine content equivalent to the daily caffeine intake of the individual. This level of caffeine is reduced while the level of analgesia is increased. The relevant proportion of caffeine is gradually decreased until the individual is no longer ingesting caffeine. In some embodiments, a placebo is administered during the final stages of method and system.

Abstract: The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

Abstract: There is described a process for the preparation of a compound of formula I ##STR1## in which process: a) a compound of formula II ##STR2## is reacted with an organolithium compound of formula IIILi--R.sub.7 (III)b) the resulting lithium complex is reacted with a compound of formula IVY.sub.1 --CO--CO--Y.sub.1 IVto form a compound of formula V ##STR3## c) that compound is, in either order, c1) oximated with O-methylhydroxylamine; or oximated with hydroxylamine and then methylated or fluoromethylated or difluoromethylated;c2) reacted with a chloroformic acid ester.X, m, Y, R.sub.1 to R.sub.3 and R.sub.7 are as defined in the description.

Abstract: Described are preferred processes for hydrolyzing substituted and unsubstituted cyanopyridines in the presence of a base and under substantially adiabatic conditions to produce pyridine substituted amides and/or pyridine substituted carboxylic acids. Preferred processes can be conducted in a variety of continuous reactors including cascades of reaction vessels, loop reactors or flow tube reactors. More preferred are the efficient and advantageous preparations of nicotinamide and niacin, which serve as important members of the B-vitamin complex.

Abstract: The invention relates to a process for the preparation of 1-hydroxy-2-pyridones of the formula I ##STR1## by reaction of a pyrone of the formula II ##STR2## with a hydroxylammonium salt in the presence of basic compounds, which comprises carrying out the reaction in the presence of a distillable, filterable or extractable acid or a salt thereof in an amount of 0.01 to 20 equivalents with respect to the pyrone of the formula II, and employing as the basic compounds an alkali metal carbonate and/or alkali metal bicarbonate in an amount of 0.8 to 5 equivalents with respect to the hydroxylammonium salt, the radicals R.sup.1 and R.sup.2 in the formulae I and II are described herein.

Abstract: Disclosed are improved processes for the recovery of 3,4-epoxy-1-butene (epoxybutene) from an epoxidation effluent comprising epoxybutane, butadiene, oxygen and an inert diluent obtained by the selective epoxidation of butadiene with an oxygen-containing gas in the presence of a catalyst and an inert gas. Epoxybutene is separated from the effluent by means of an absorption process using an extractant comprising liquid butadiene and, optionally, a hydrocarbon diluent. The formation of butenediols, by the reaction of epoxybutene and water, in the recovery process is inhibited by the addition of a base, preferably an alkali metal base, to the recovery system.

Abstract: This invention relates to a phenylene derivative represented by the following formula (1) or a salt thereof and also to a medicine containing it as an effective ingredient. ##STR1## wherein R.sup.1 represents H or halogen; A represents --CH.dbd.CH--, --CH.dbd.N--, --N(R.sup.2)--, --O-- or --S--; W represents --CH.dbd.CH-- or --CH.sub.2 O--; X represents --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 N(R.sup.3)--, --CH.dbd.N--, --COO-- or --CONH--; Y represents ##STR2## B.sup.1 represents --C(R.sup.7)(R.sup.8)(CH.sub.2).sub.l --, --S(O).sub.m (CH.sub.2).sub.n -- or --CH.dbd.C(R.sup.9)--; B.sup.2 represents --CH.sub.2 CH.sub.2 -- or --CH.sub.2 CH.sub.2 CH.sub.2 --; Z.sup.1 and Z.sup.2 each represents O or S; etc. The phenylene derivative or salt thereof has antileukotrienic action and antihistaminic action and is useful as a medicine such as an asthma preventive or curative.

Abstract: A process for the production of a phenol derivative of the formula (2), which comprises subjecting a diester compound of the formula (1) in which a hydroxyl group is protected by an acyl group, to a reaction for removal of protection, wherein the reaction is carried out in the presence of an aliphatic amine as a protection-removal agent, ##STR1## wherein X is hydrogen or fluorine, Y is --CH.sub.3 or --CF.sub.3, Q is an alkyl group having 1 to 4 carbon atoms, p is 0 or 1, m is an integer of 2 to 7, n is an integer of at least 1, and C* is an asymmetric carbon,the process enabling to obtain the phenol derivative of the formula (2) useful as an intermediate for a liquid crystal compound with ease and at high purity.

Abstract: New compounds of the formula (A) ##STR1## a process for their preparation and their use in the manufacture of pharmaceutical preparations. The new compounds have both local anaesthetic and analgesic effect.

Abstract: Provided herein are novel syntheses of the phosphate-based inositol derivatives 1-O-?(+)-menthoxycarbonyl!-6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inos itol (D4P), D-myo-inositol 1,4,5-trisphosphate (D-IP.sub.3), 6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inositol H-phosphonate ((-)-3-HP) and L-myo-inositol 1,4,5-trisphosphate (L-IP.sub.3). These syntheses employ fewer column chromatography steps for the isolation of intermediates than do prior art syntheses, and hence, are more convenient, economical and efficient than are the previously known synthetic methods.

Abstract: Compounds selected from the series consisting of the perylenecarboximide, quinacridone, isoindoline, indigoid, azo, benzodipyrrolone, benzodifuranone, furanofuran, pyrrolo?2,5-b!pyrrole and bianthraquinone chromophores containing at least one grouping of formula ##STR1## wherein each A may be N--CN or O, with the proviso that at least one A must be N--CN, X is --N(R)--, --O-- or --S--, R is hydrogen, C.sub.1 -C.sub.18 alkyl, unsubstituted or halogen- or C.sub.1 -C.sub.4 alkyl-substituted phenyl, benzyl or phenethyl, and m and n are each independently of the other 0 or 1.Depending on the nature of their substituents, these compounds can be used as polymer-soluble dyes or as pigments for coloring high molecular weight organic material. They are distinguished by a surprisingly high solid-state fluorescence.

Abstract: Photoconductive imaging members comprised of unsymmetrical dimeric perylene as a charge generator, wherein said perylene is of the following formula ##STR1## wherein R is hydrogen, alkyl, cycloalkyl, substituted alkyl, aryl, substituted aryl, aralkyl or substituted aralkyl group, and X--Y is an unsymmetrical bridging moiety of alkylene, substituted alkylene, arylene, substituted arylene, aralkylene or substituted aralkylene.

Abstract: Novel 1H-imidazo?4,5-c!quinolin-4-amines are disclosed. The compounds function as antiviral agents and they are potential synthetic intermediates in the preparation of known antiviral agents and labeled known antiviral agents. Processes for the preparation of the compounds, methods for their antiviral use, and methods of inducing interferon biosynthesis, are also described.

Abstract: A process for producing optically active 2-halo-1-(substituted phenyl)ethanol of a formula (Ia) or optically active styrene oxide of a formula (Ib). The process comprises the steps of reacting a compound of a formula (II) with phthalic anhydride to give a compound of a formula (III), performing optical resolution on the resulting compound using an optically active organic amine as a resolving agent, and finally performing hydrolysis or alcoholysis on the optically resolved compound (Ia) or (Ib). The scheme of the above process is: ##STR1## wherein X represents a halogen atom, Y represents a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a C.sub.1 -C.sub.6 haloalkyl group or a C.sub.1 -C.sub.6 haloalkoxy group, Z represents a hydrogen atom, a halogen atom or a C.sub.1 -C.sub.6 alkyl group, n is 0 or an integer of 1 to 3 and m is 0 or an integer of 1 to 2. The resulting optically active compounds are useful as an intermediate for medicines.

Abstract: Disclosed are an improvement of a process for the preparation of a purified 3,4-epoxycyclohexyl methyl(meth)acrylate, and a stabilized 3,4-epoxycyclohexyl methyl(meth)acrylate.

Abstract: N-heterocyclic moiety containing hydroxyethylamine compounds of the formula: ##STR1## such as 3-isoquinolinecarboxamide,N-(,1-dimethylethyl)decahydro-2-?2-hydroxy-3-??2 -methyl-3-(methysulfonyl)-1-oxopropyl!amino!-4-phenylbutyl!-, ?3S-?2?2S*,3R*(R*)!,3.alpha.,4a.beta., 8 a.beta.!!- are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.