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1. WO1996004253 - PROCESSES AND INTERMEDIATES IN THE SYNTHESIS OF 5-(3-[EXO-BICYCLO[2.2.1]HEPT-2-YLOXY]-4-METHOXYPHENYL)-3,4,5,6-TETRAHYDROPYRIMIDIN-2(1H)-ONE

Publication Number WO/1996/004253
Publication Date 15.02.1996
International Application No. PCT/IB1995/000319
International Filing Date 04.05.1995
Chapter 2 Demand Filed 10.08.1995
IPC
C07C 69/734 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
66Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, -CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
73of unsaturated acids
734Ethers
C07C 235/34 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
32the carbon skeleton containing six-membered aromatic rings
34having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 255/37 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
01having cyano groups bound to acyclic carbon atoms
32having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
37the carbon skeleton being further substituted by etherified hydroxy groups
C07C 259/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
259Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
06having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 271/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
16to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
C07C 271/20 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
20to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
CPC
C07C 235/34
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
02having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
32the carbon skeleton containing six-membered aromatic rings
34having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 255/37
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
255Carboxylic acid nitriles
01having cyano groups bound to acyclic carbon atoms
32having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
37the carbon skeleton being further substituted by etherified hydroxy groups
C07C 259/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
259Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
06having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 2603/70
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2603Systems containing at least three condensed rings
56Ring systems containing bridged rings
58containing three rings
70containing only six-membered rings
C07C 271/16
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acids, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
16to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
C07C 271/20
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acids, i.e. compounds containing any of the groups , the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
10with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
20to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
Applicants
  • PFIZER INC. [US/US]; 235 East 42nd Street New York, NY 10017, US (AllExceptUS)
  • LACOUR, Thomas, G. [US/US]; US (UsOnly)
  • MURTIASHAW, Charles, W. [US/US]; US (UsOnly)
Inventors
  • LACOUR, Thomas, G.; US
  • MURTIASHAW, Charles, W.; US
Agents
  • SPIEGEL, Allen, J.; Pfizer Inc. Patent Dept. 235 East 42nd Street New York, NY 10017, US
Priority Data
08/286,57905.08.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESSES AND INTERMEDIATES IN THE SYNTHESIS OF 5-(3-[EXO-BICYCLO[2.2.1]HEPT-2-YLOXY]-4-METHOXYPHENYL)-3,4,5,6-TETRAHYDROPYRIMIDIN-2(1H)-ONE
(FR) PROCEDES ET INTERMEDIAIRES PERMETTANT LA SYNTHESE DE 5-(3-[EXO-BICYCLO[2.2.1]HEPT-2-YLOXY]-4-METHOXYPHENYL)-3,4,5,6-TETRAHYDROPYRIMIDIN-2(1H)-ONE
Abstract
(EN)
This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.
(FR)
L'invention concerne de nouveaux procédés permettant de préparer le composé pharmaceutiquement actif 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-méthoxyphenyl)-3,4,5,6-tétrahydropyrimidin-2(1H)-one et son énantiomère 2R correspondant, ainsi que de préparer certains intermédiaires utilisés dans la synthèse de tels composés. L'invention concerne également de nouveaux intermédiaires utilisés dans la synthèse de tels composés pharmaceutiquement actifs, ainsi que d'autres nouveaux composés apparentés à de tels intermédiaires.
Also published as
FI970470
NO19970497
NO20000404
NO20003899
NZ284144
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