Abstract: Novel processes are disclosed for the preparation and resolution of substituted piperidines of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined as below, and related compounds, as well as novel intermediates used in such processes.
Type:
Grant
Filed:
July 12, 1994
Date of Patent:
September 2, 1997
Assignee:
Pfizer Inc
Inventors:
Terry J. Rosen, Dennis M. Godek, Sally Gut, Lewin Wint
Abstract: The present invention relates to a novel process for the preparation of highly potent histamine receptor antagonists, in particular histamine H.sub.3 -receptor antagonists. Also disclosed is a novel process for the preparation of intermediates useful in the preparation of histamine receptor antagonists, in particular H.sub.3 -receptor antagonists.
Abstract: A process for the preparation of the compound of formula (I) ##STR1## or a salt thereof which comprises reducing the compound of formula (II) ##STR2## or a salt thereof. The novel intermediate of formula (II) and processes for preparing it are also described.
Type:
Grant
Filed:
February 29, 1996
Date of Patent:
August 19, 1997
Assignee:
Glaxo Group Limited
Inventors:
Philip Blatcher, Malcolm Carter, Roy Hornby, Martin Richard Owen
Abstract: The invention relates to a new process for the preparation of benzyl-piperidylmethyl-indanones known as medicaments, which is characterized in that the appropriately substituted pyridinium salts are hydrogenated.
Abstract: A process for the preparation of 2-aminomethylpiperidine by catalytic hydrogenation of 2-cyanopyridine in the presence of a cobalt-containing catalyst at elevated temperature and under elevated pressure. The reaction can be carried out either in two steps or in a single stage.
Type:
Grant
Filed:
September 23, 1992
Date of Patent:
December 20, 1994
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Detlef Kampmann, Gregor Deckers, Claus Kniep
Abstract: The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R.sup.1 is a six membered saturated or unsaturated heterocyclic ring containing one or two heteroatoms wherein the heteroatoms are N; or NR.sup.6, wherein R.sup.6 is H or C.sub.1-10 alkyl;m is an integer from two to six; andR.sup.4 is aryl, C.sub.1-10 alkyl, or C.sub.4-10 aralkyl.
Type:
Grant
Filed:
February 16, 1993
Date of Patent:
May 17, 1994
Assignee:
Merck & Co., Inc.
Inventors:
John Y. L. Chung, David L. Hughes, Dalian Zhao
Abstract: A process for preparing a compound of formula (I): ##STR1## in which Ar represents an aryl or substituted aryl group and R.sup.3 represents an alkyl group, which comprises reducing a compound of formula (II): ##STR2## in which Ar and R.sup.3 are as defined for formula (I), and Hal represents a halogen atom.
Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.
Abstract: A process is disclosed for the preparation of a compound of formula (I): ##STR1## where Ar is aryl or substituted aryl and R.sup.3 and R.sup.4 are the same or different and each is alkyl, which process comprises hydrognating a compound of formula (II): ##STR2## wherein Ar, R.sup.3 and R.sup.4 are as defined with respect to formula (I) and Hal is a halogen atom.Compounds of formula (I) are useful as chemical intermediates.
Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.
Abstract: A new and novel process for the preparation of encainide (4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]-benzanilide) has been developed. The process utilizes .alpha.-picoline, O-nitrobenzaldehyde, and anisoyl chloride as starting materials.
Abstract: Nitroaryl carbonyl Formula (IIA) compounds, their nitrodihydroaryl carbonyl Formula (I) intermediates, processes for preparing Formula (II) compounds, and a process for preparing Formula (I) compounds, wherein each process comprises the reaction of a nitroaryl compound with a silane.
Abstract: The present invention relates to processes for preparing precursors of picenadol, (.+-.)3-(1,3.alpha.-dimethyl-4.alpha.-propyl-4.beta.-piperidinyl)phenol, hydrochloride, a known analgesic. Certain of the compounds prepared by the present process are novel as well.
Abstract: An improved process for the preparation of 4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]benzanilide has been developed. The process comprises essentially three steps starting with methyl anthranilate and 2-picoline and features a novel low-pressure hydrogenation sequence.
Abstract: A process for the preparation of 1-(4-hydroxyphenyl)-2-(4-benzylpiperidino)-1-propanol (i.e. ifenprodil) and acid-addition salts thereof, characterized by brominating 4'-hydroxypropiophenone in a single or mixed solvent selected from the group consisting of methanol, ethanol and a saturated aliphatic ether, removing hydrogen bromide formed in the course of the bromination, adding 4-benzylpyridine to the reaction mixture, heating the reaction mixture under reflux in a single or mixed solvent selected from the group consisting of methanol and ethanol, and then subjecting the resultant reaction mixture to catalytic reduction to form 1-(4-hydroxyphenyl)-2-(4-benzylpiperidino)-1-propanol hydrobromide in the reaction mixture. The end product (i.e.
Abstract: An improved process for the preparation of pyridines and/or hydrogenated pyridines that have been substituted with a hydrocarbon group at one or more carbon atoms, .gamma.-cyanoketone, in a gaseous phase and in the presence of hydrogen, is passed in a reaction zone over a first catalyst containing a catalytically active metal or compound of a metal selected from the group copper, silver, gold, iron, nickel, cobalt, ruthenium, rhodium, palladium, osmium, iridium and platinum to form a reaction mixture. A hydrogen-containing gas is separated from the reaction mixture, passed over a second catalyst containing a catalytically active metal or compound of a metal selected from the group iron, nickel and cobalt at a temperature of between 300.degree. and 800.degree. C., and the hydrogen-containing gas so treated is recycled to the reaction zone.
Type:
Grant
Filed:
September 19, 1979
Date of Patent:
June 30, 1981
Assignee:
Stamicarbon, B.V.
Inventors:
Egidius J. M. Verheijen, Charles H. Geersheuvels
Abstract: 2-(2,2-Dicyclohexylethyl)piperidine is prepared via the catalytic hydrogenation of 2-(2,2-diphenylethenyl)pyridine in a single step. High yields are obtained using a rhodium supported catalyst.
Type:
Grant
Filed:
April 14, 1976
Date of Patent:
March 4, 1980
Assignee:
Richardson-Merrell Inc.
Inventors:
Stephen W. Horgan, Frank P. Palopoli, David L. Wenstrup