Abstract: In the preparation of a 4-hydroxycinnoline wherein the diazonium salt of a 2-aminoacetophenone in aqueous solution is allowed to undergo cyclocondensation, the improvement that comprises maintaining the pH of the solution between about 4.0 and 8.5 during the cyclocondensation.
Abstract: This disclosure relates to a method and reagents for determining ligands in biological fluids such as serum, plasma, spinal fluid, amnionic fluid and urine. This disclosure also relates to a novel class of tracer compounds employed as reagents in fluorescence polarization immunoassays.
Type:
Grant
Filed:
July 11, 1984
Date of Patent:
September 30, 1986
Assignee:
Abbott Laboratories
Inventors:
Curtis L. Kirkemo, Mohammed T. Shipchandler
Abstract: .beta.-N-aziridinopropionates of relatively high boiling alcohols or polyalcohols are prepared by transesterifying a .beta.-N-aziridinopropionate of a lower alcohol of 1 to 4 carbon atoms with a relatively high boiling alcohol or polyalcohol by a process in which the transesterification is carried out in the presence of, as a transesterification catalyst, a titanium(IV) or tin(IV) compound which is soluble in an organic medium.
Type:
Grant
Filed:
July 9, 1984
Date of Patent:
September 30, 1986
Assignee:
BASF Aktiengesellschaft
Inventors:
Rolf Fikentscher, Siegfried Schneider, Erhard Klahr, Friedrich Reinert, Gunter Eckert, Adolf Stuebinger
Abstract: Process for the preparation of .alpha.-chlorinated chloroformates with the formula ##STR1## where R is H, an aliphatic or aromatic hydrocarbon radical or heterocyclic radical, substituted or non-substituted and n an integer.The process consists of reacting ClCOOCCl.sub.3 or Cl.sub.3 COCOOCCl.sub.3 with an aldehyde with formula R--(CHO).sub.n in the presence of a compound, which in the medium releases a pair of ions, the anion of which being a halide which can attack the aldehyde function, because of the weak attractive power of the cation of this compound.
Type:
Grant
Filed:
August 17, 1984
Date of Patent:
September 30, 1986
Assignee:
Societe Nationale des Poudres et Explosifs
Inventors:
Thierry A. Malfroot, Jean-Pierre G. Senet
Abstract: 2,4-Diamino-6-halogeno-5-alkylthio-pyrimidines of the general formula (I) ##STR1## in which X represents halogen,R.sup.1 represents alkyl which is optionally substituted by halogen,R.sup.2 represents hydrogen or alkyl,R.sup.3 represents hydrogen, alkyl or alkoxyalkyl,R.sup.4 represents hydrogen or alkyl,Z represents a branched or straight-chain alkylene group andR.sup.5 represents alkyl,process for their preparation and their use as plant protecting agent, particularly as herbicides and fungicides.
Type:
Grant
Filed:
May 3, 1985
Date of Patent:
September 30, 1986
Assignee:
Bayer Aktiengesellschaft
Inventors:
Michael Schwamborn, Engelbert Kuhle, Erich Klauke, Ludwig Eue, Robert R. Schmidt, Hans-Joachim Santel, Gerd Hanssler
Abstract: A compound of the Formula (I): ##STR1## where X is a benzyl group or a benzyloxybenzyl group and pharmaceutical preparations containing the same.
Type:
Grant
Filed:
July 31, 1985
Date of Patent:
September 23, 1986
Assignee:
Brown University Research Foundation
Inventors:
Shih H. Chu, Paul Calabresi, Ming Y. W. Chu, Mahmoud H. el Kouni, Fardos N. M. Naguib, Sungman Cha
Abstract: A process for the preparation of fluoroformates of formula: ##STR1## in which R.sup.1 is a substituted or unsubstituted, saturated or unsaturated aliphatic, cycloaliphatic or polycyclic radical, or substituted or unsubstituted araliphatic radical or an aromatic radical, which consists of reacting a carbonate of formula: ##STR2## in which R.sup.1 has the same meaning as hereinabove and R.sup.2 is hydrogen, alkyl of 1-12 carbon atoms, cycloalkyl of 5-12 carbon atoms, saturated or unsaturated, unsubstituted or substituted by one or more halogen atoms or R.sup.2 is aryl, unsubstituted or substituted by one or more halogen atoms, with an alkali or alkaline earth fluoride, ammonium fluoride or a quaternary ammonium fluoride, of formula FNR.sup.3 R.sup.4 R.sup.5 R.sup.6, wherein R.sup.3, R.sup.4, R.sup.5, R.sup.6 are the same or different and are hydrogen, alkyl or aralkyl of 1-12 carbon atoms or a fluoride which is KHF.sub.2, NH.sub.4 HF.sub.2 or KSO.sub.2 F.
Type:
Grant
Filed:
September 17, 1984
Date of Patent:
September 16, 1986
Assignee:
Societe Nationale des Poudres et Explosifs
Inventors:
Marc Piteau, Jean-Pierre Senet, Patrick Wolf, Roy A. Olofson, Vu A. Dang
Abstract: A process for the preparation of pyrimidinetrione derivatives of formula (I) is described ##STR1## wherein R.sup.1 and R.sup.2, which may be the same or different, represent aliphatic, araliphatic or aryl groups, and R.sup.3 represents a group of the formula --CH.sub.2 CH(OCONH.sub.2)--CH.sub.2 OX wherein X is hydrogen or a C.sub.1-5 alkyl group which comprises reacting approximately equimolar amounts of a monoalkali metal salt of a compound of formula (I), wherein R.sup.3 is a hydrogen atom, with an alkylating agent R.sup.3 Hal wherein R.sup.3 is as defined above and Hal represents a halogen atom, in the presence of at least 0.2 moles of an acid of formula (I) wherein R.sup.3 is a hydrogen atom per mole of alkali metal salt. The yield is increased by up to 50% by this method. The process is of particular application to the preparation of febarbamate, 1-(3-.sup.n butoxy-2-carbamoyloxypropyl)-5-ethyl-5-phenyl-(1H, 3H,5H)pyrimidine-2,4,6-trione.
Type:
Grant
Filed:
April 11, 1984
Date of Patent:
September 9, 1986
Assignee:
Sapos S.A.
Inventors:
Philippe Gold-Aubert, Diran Melkonian, Jindrich Vachta, Karel Valter, Bernard Siegfried, Stephane Hugentobler
Abstract: An improved process for the preparation of aromatic carbonates selected from aliphatic aromatic carbonates and diaromatic carbonates comprising reacting at least one phenolic compound with at least one dialiphatic carbonate or at least one aliphatic aromatic carbonate in the presence of a catalytic amount of a catalyst comprised of (i) at least one Lewis acid, and (ii) at least one protic acid.
Abstract: Carboxy-thiazolo[3,2-a]pyrimidine derivatives, and pharmaceutical compositions containing them. The compounds and compositions possess anti-allergic activity.
Type:
Grant
Filed:
June 21, 1985
Date of Patent:
September 2, 1986
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Carlo Passarotti, Maria L. Corno
Abstract: Novel 2-guanidinothiazoline compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, and the acid addition salts thereof; they are important intermediate compounds for preparing famotidine and thiotidine which are medicaments useful as gastric acid secretion inhibitors.
Abstract: The present invention provides aryloxypropanolamines of the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, are hydrogen or halogen atoms or lower alkyl, cyano, carboxamide, hydroxyl, lower acyloxy, lower alkoxy, lower alkenyloxy or aryl lower alkoxy radicals, R.sub.5 and R.sub.6, which may be the same or different, are hydrogen atoms or lower alkyl radicals, X is a straight or branched alkylene chain containing 2 to 6 carbon atoms, A is a mono-, bi- or tricyclic heteroaromatic or hydroheteroaromatic radical or, when at least one of the symbols R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is other than a hydrogen atom, may also be a phenyl radical, with the proviso that when A is a uracil-6-yl radical, the 5-position of the uracil moiety does not contain a hydrogen atom, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.
Type:
Grant
Filed:
October 3, 1983
Date of Patent:
August 26, 1986
Assignee:
Boehringer Mannheim GmbH
Inventors:
Fritz Wiedemann, deceased, Wolfgang Kampe, Karl Dietmann, deceased, Gisbert Sponer
Abstract: Novel 4-substituted-5-hydroxymethyl-1,2-cyclopentanediols or 1-cyclopentanol substituted at the 3-position by various heterocyclic groups are useful as antiviral agents.
Type:
Grant
Filed:
April 30, 1985
Date of Patent:
August 12, 1986
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Julien P. H. Verheyden, John C. Martin, G. V. Bindu Madhaven, Daniel P. C. McGee, Ernest J. Prisbe
Abstract: Highly selective and high yield process for producing antitumor agent 1-phthalidyl-5-fluorouracil derivatives of formula (I) which comprises reacting a phthalidyl compound (II) with an amine (III) to yield the quaternary ammonium salts (IV), and reacting the latter with 5-fluorouracil. ##STR1## [wherein X is leaving group; ##STR2## is triethylamine, N-methylmorpholine, N-ethylmorpholine, and the like; R.sup.4 and R.sup.5 each is hydrogen, trialkylsilyloxy, alkoxy, nitro, cyano, carboxy, or alkoxycarbonyl].
Abstract: Piperidino-substituted pyrimidines which are intermediates for preparing piperidino-substituted imidazo-[1,5-c]pyrimidines which are bronchodilators.
Abstract: This invention is a process for the preparation of a symmetrical or unsymmetrical dihydrocarbyl carbonate which comprises contacting an aliphatic, cycloaliphatic or di(aryl-substituted aliphatic) alcohol or mixtures thereof with carbon monoxide and oxygen in the presence of a catalytic amount of bis((2,4-pentanedianato)copper (II) methoxide) and a cocatalytic amount of a basic nitrogen-containing coordination compound under conditions such that a symmetrical or unsymmetrical dihydrocarbyl carbonate is prepared.
Type:
Grant
Filed:
March 19, 1984
Date of Patent:
August 5, 1986
Assignee:
The Dow Chemical Company
Inventors:
A. Dale Harley, Jerald L. Curnutt, David T. Doughty
Abstract: A pigmentary form of isoindoline pigments which has high color strength is obtained if these pigments contain(a) a compound of the formula (I) ##STR1## and (b) one or more isoindoline compounds of the formula (II) ##STR2## and the pigment is obtained by dry-blending (I) and (II) until the primary particles are .ltoreq.0.2 .mu.m and then heating the finished mill base in an organic liquid or in a mixture of water and an organic liquid. In the formulae, X is ##STR3## and R.sup.2 is --CN, --CONHR.sup.4, 2-quinazolonyl, 2-quinoxazolonyl or 2-benzimidazolyl, R.sup.3 is hydrogen, alkyl or unsubstituted or substituted phenyl, R.sup.1 is hydrogen or methyl, and R.sup.4 is hydrogen, alkyl or phenyl, and the phenyl radical and/or the heterocyclic radicals can be further substituted. The compounds I and II differ from one another.The color strengths of the resulting pigments are substantially superior to the prior art.
Abstract: A novel compound, useful as an intermediate in the production of compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sub.a.sup.1 is hydrogen, amino or a protected amino group,R.sub.b.sup.1 and R.sub.c.sup.1 are each hydrogen, halogen, lower alkoxy or arylthio,R.sup.14 is carboxy or a protected carboxy group,X is lower alkylene or a group of the formula: ##STR2## in which R.sup.6 is hydrogen or an organic residue which may have suitable substituent(s), andZ is N or CH,or a salt thereof.
Abstract: 1'-Ethoxycarbonyloxyethyl ester of di-n-propylacetic acid, also known as valproic acid. The novel compound is prepared by reacting valproic acid with 1-haloethyl ethyl carbonate. There are also provided pharmaceutical compositions for oral administration containing the said ester.
Type:
Grant
Filed:
November 16, 1983
Date of Patent:
June 17, 1986
Assignee:
Teva Pharmaceutical Industries Ltd.
Inventors:
David Ladkani, Haim Yellin, Ben Z. Weiner