Abstract: N-ethoxycarbonyl-14-hydroxynorcodeinone is prepared by contacting N-ethoxycarbonyl-norcodeinone enol acetate with an aromatic or aliphatic mono-basic or poly-basic peroxy-acid under reaction conditions effective for substituting an --OH group in the 14-position of the norcodeinone enol acetate.In a preferred embodiment the reaction conditions include effecting the contacting in the presence of (A) a moderately strong acid having a pK.sub.a of from about 0.3 to about 3.5, (B) an inert organic solvent, and (C) in the substantial absence of water.Codeine is converted to noroxymorphone by an improved process employing the above method for introducing the 14-hydroxy group into the codeine derivative.
Abstract: Disclosed is a process for inhibiting polymerization of polymerizable ethylenically unsaturated monomers such as hydrocarbons, acids and esters, wherein a cobalt (III), nickel (II) or manganese (II) complex of N-nitrosophenylhydroxylamine is employed. A composition including a polymerizable ethylenically unsaturated monomer and the complex is also disclosed. In a preferred embodiment, polymerization of an acrylic acid or an acrylate ester is inhibited.
Abstract: Polyol carboxyalkylthioalkanoamidophenol compounds useful in the stabilization of organic materials normally susceptible to oxidative degradation are prepared by (A) reaction of an appropriate polythiol, which is a selected tetra-(mercapto alkanoic acid) ester of pentaerythritol or a selected tri-(mercapto alkanoic acid) ester of a selected 1,1,1-trimethylolalkane, with an appropriate alkenyl compound, which is a selected N-alkenoyl[4-amino(mono- or dialkyl)phenol] or (B), where the alkanol moiety is a sole methylene group, by reaction of pentaerythritol or an appropriate 1,1,1-trimethylolalkane with an appropriate mercapto-N(mono- or di-alkyl-4-hydroxyphenylalkamide) alkanoic acid. In a preferred embodiment, the compound is pentaerythritol tetrakis[3-mercapto-N-(3',5'-di-ti-butyl-4'-hydroxyphenyl propanamide) propionate].
Type:
Grant
Filed:
August 20, 1985
Date of Patent:
January 6, 1987
Assignee:
Mallinckrodt, Inc.
Inventors:
Neil Dunski, Ali A. Bazzi, Henry J. Buehler
Abstract: Disclosed are an acetaminophen composition containing a minor amount of a pheniramine maleate, a spray-drying method for preparing the composition and orally administerable analgesic antihistaminic tablets formed from the composition.
Abstract: An N-acetyl-p-aminophenol composition capable of being directly formed into a tablet having high hardness, short disintegration time and short dissolution time is disclosed. The composition includes N-acetyl-p-aminophenol, a pharmaceutically acceptable partially gelatinized starch, a pharmaceutically acceptable lubricant, water and optionally an auxiliary binder, an auxiliary disintegrant or both of these optional components. Also disclosed is a method for preparing the essential components (and optional components if desired) and spray drying the slurry.
Type:
Grant
Filed:
June 7, 1983
Date of Patent:
July 15, 1986
Assignee:
Mallinckrodt, Inc.
Inventors:
Anil M. Salpekar, Steven R. Freebersyser, Douglas A. Robinson
Abstract: The invention relates to radiolabelled metallocene derivatives of the general formula ##STR1## wherein Mc is a metallocenyl group with a radioactive central atom,R is a carbonyl or methylene group,R.sub.1 is a hydrogen atom or an alkyl group having 1-4 carbon atoms,A is a carboxy group or a pharmaceutically acceptable salt thereof, or an alkoxycarbonyl or alkanoyl group having 2-5 carbon atoms, andn is 1-4.The invention also relates to radiodiagnostic compositions comprising said radiolabelled metallocene derivatives and to a method of performing a radiodiagnostic examination, in particular of examining the renal function.
Abstract: Bis(aminophenyl) ethers are prepared by effecting condensation reaction of an (N-acetyl)aminophenol or the corresponding sodium or potassium (N-acetyl)aminophenate with a halonitrobenzene under condensation reaction conditions to form an (N-acetyl)aminophenylnitrophenyl ether and hydrogenating the nitro group thereof under nitro- group hydrogenation conditions to form an (N-acetyl)bis(aminophenyl) ether. The latter compound is hydrolyzed with aqueous mineral acid under acid hydrolysis conditions to form an acidic aqueous dispersion of the bis(aminophenyl) ether product, which can readily be recovered from the disperson. Final bis(aminophenyl) ether products thus prepared are typically of high purity and excellent color properties, i.e., substantially colorless.
Abstract: Diaminodiphenyl ethers (DADPE's) are prepared by refluxing sodium or potassium aminophenate with chloronitrobenzene in dimethylformamide. The reaction mixture is hydrogenated directly without isolating the resulting intermediate product, aminophenyl-nitrophenyl ether, to form the corresponding DADPE, e.g., oxydianiline (ODA). The DADPE is crystallized from the hydrogenated reaction mixture in the presence of an aliphatic alcohol, which may be added to the reaction mixture prior to, during, or after hydrogenation. The resulting crystallized DADPE is typically of high purity and excellent color.
Abstract: A salt of 3,4,5-trimethoxybenzoic acid is prepared by initially reacting hydrolyzable tannin with a methylation agent in an alkaline medium under methylation conditions to form methylated tannin and thereafter hydrolyzing the methylated tannin by reaction thereof with a hydrolysis agent under alkaline hydrolysis conditions. The resulting salt can be neutralized to form 3,4,5-trimethoxybenzoic acid, which can readily be recovered.
Abstract: Radioimunoassay methods for determining the concentration of fibrinopeptide A in plasma, anticoagulation reagents for use in such methods and package test kits containing the reagents for use in such methods are provided.
Abstract: This invention relates to a process for treating Limulus Lysate having improved sensitivity to endotoxin, to lysate reagents utilizing such lysate, and to the use of such lysate reagents.
Abstract: Ethylene is polymerized in the vapor phase in a stirred bed reactor. The reactor employed is vertically aligned and has a centrally positioned cored draft tube therein. An auger circulates polymer solids through the draft tube while coolant is circulated there through to remove the heat of polymerization.