American Cyanamid Company

Wyeth

Karykion Corporation

Arthur G Mohan

Michael M Rauhut

John Potoski

Panolil C Raveendranath

Silvio Iera

Sreenivasulu Megati

Galina Vid

Maria Papamichelakis

Christopher Demerson

Wayne G McMahon

Joseph D'Antuono, Iii

Jacqueline F Lunetta

Michael F MacEwan

David Michael Blum

Shin-Shyong Tseng

Robert J Manfre

Antonia Nikitenko

This invention relates to a process for the preparation of 6-hydroxyequilenins, which are useful as estrogenic agents.

Preparation of 6-hydroxyequilenins

The present invention provides a new process and intermediates for the production of antiviral compound 4',4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2&#x2032;-disulfonic acid and its pharmaceutically acceptable salts.

Preparation and purification of antiviral disulfonic acid disodium salt

The present invention provides a new process and intermediates for the production of antiviral compound 4&prime;,4-bis-&lcub;4,6-bis-&lsqb;3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino&rsqb;-&lsqb;1,3,5&rsqb;triazin-2-ylamino&rcub;-biphenyl-2,2&prime;-disulfonic acid and its pharmaceutically acceptable salts.

Processes for the preparation of high purity alkyl esters of polyene macrolide antibiotics are disclosed. The processes involve treating an amphoteric polyene macrolide antibiotic with an aldehyde to yield the corresponding Schiff base which is soluble in the reaction medium. The solution is then treated with an alkylating agent in the presence of a hindered tertiary amine as acid acceptor to yield the alkyl ester of the polyene macrolide antibiotic in the form of its Schiff base derivative. Contacting this derivative with water converts the Schiff base derivative to the desired alkyl ester of the polyene macrolide antibiotic which is recovered from the reaction medium.

Polyene macrolide schiff bases, their alkyl esters and processes for

A process for the regioselective N-alkylation of 2-alkyl-5,6,7 or 8-substituted-4(3H)-quinazolinones in the presence of lithium salts.

Process for the regioselective n-alkylation of quinazolinones

The invention is the simultaneous addition of boron tribromide and a solution of [R-(R*,R*)]-5-(3-chlorophenyl-3-[2-(3,4-dimethoxyphenyl)-1-methylethyl]-2- oxazolidinone in methylene chloride to methylene chloride while maintaining a constant ratio of 2.10:1.00 of boron tribromide to the substrate [R-(R*,R*)]-5-(3-chlorophenyl-3-[2-(3,4-dimethoxyphenyl)-1-methylethyl]-2- oxazolidinone at a temperature of -5.degree. C. to 10.degree. C. gives [R-(R*,R*)]-5-(3-chlorophenyl-3-[2-(3,4-hydroxyoxyphenyl)-1-methylethyl]-2 -oxazolidinone in an isolated yield of 86.7% and a purity of 98.7%.

Process for the synthesis

A novel process for producing 2-alkyl-3,5,6,7 or 8-substituted-4 (3H)-quinazolinones of the formula: ##STR1## where R, R.sup.1 and R.sup.2 are defined in the specification by reacting the appropriately N-acyl substituted aminobenzoic acids with ethylchloroformate followed by further reaction with ammonia or a primary amine.

Process for the preparation of 2-alkyl-3,5,6,7- or

In chemical light devices comprising a chemi-luminescent mixture with a first fluorescer contained in a transparent or translucent container, a second fluorescer is incorporated in the walls of the container to shift at least part of the emissions from the device from the shorter wavelength emission of the first fluorescer to a longer wavelength emission of the second fluorescer. The second fluorescer has an absorption spectrum substantially overlapping the emission spectrum of the first fluorescer. The shift is usually about 20 to 100 nanometers and may be as much as 200 nanometers.

Chemical lighting device

Water-soluble sulfonated rubrenes are used as fluorescer components in water-soluble chemiluminescent mixtures and particularly in combination with a water-soluble amide of oxalic acid which reacts with hydrogen peroxide to produce chemiluminescence.

Sulfonated rubrene and aqueous chemiluminescent compositions containing

An improved single-pot process for synthesis of 3,5,6-trichlorosalicylic acid and esters thereof is described. Salicylic acid is chlorinated first in concentrated sulfuric acid and then with iodine catalyst to make the trichlorosalicylic acid which is extracted and then reacted with an alcohol to make the ester.

Processes for preparing 3,5,6-trichlorosalicylic acid and esters thereof

N,N'-bis(trifluoromethylsulfonyl)oxamides are described with a number of variations by substitution at the amido nitrogen atoms. These compounds when used in chemiluminescent formulations will furnish superior light intensity and quantum efficiency. Preparation of compounds and their use for chemiluminescence are described.

N,N-Bis(trifluoromethylsulfonyl)oxamides and chemiluminescent

Process for preparing known classes of 2-substituted azoles (I) and N-acylazolinones (II) by reacting carbon monoxide at elevated temperature and pressure in the presence of a cocatalyst composition, of which 5% palladium on carbon with a Lewis acid such as ferric chloride is representative, with a nitrogenous compound (III): ##STR1## to form the products (usually in admixture): ##STR2## where R is alkyl, alkenyl, aralkyl, aryl, styrl or ##STR3## R.sub.1 and R.sub.2 are hydrogen, alkyl, alkoxy, aryl, halo or, when taken together on adjacent carbon atoms, -CH.dbd.CH-CH.dbd.CH-; R.sub.4 may be alkyl, alkenyl, aralkyl, aryl, styryl, ##STR4## X is oxygen, sulfur or imino, Y is alkylene, alkenylene or arylene; and Z is nitro, azo or azoxy.

Process for azoles (ring closure of nitro compounds)

This invention relates to novel water-soluble esters of oxalic acid, and to compositions that are useful for generating chemiluminescent emission by reacting said esters of oxalic acid with hydrogen peroxide in the presence of water and a fluorescent compound, and to a process for generating chemiluminescent emission by using said compositions.

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Somerville, NJ, United States of America

Arthur G Mohan