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1. WO1997028132 - PROCESS FOR PREPARING PYRIMIDIN DERIVATIVES

Publication Number WO/1997/028132
Publication Date 07.08.1997
International Application No. PCT/US1997/001860
International Filing Date 30.01.1997
Chapter 2 Demand Filed 02.09.1997
IPC
C07D 239/22 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
20having two double bonds between ring members or between ring members and non-ring members
22with hetero atoms directly attached to ring carbon atoms
C07D 239/70 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
C07D 239/90 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
86with hetero atoms directly attached in position 4
88Oxygen atoms
90with acyclic radicals attached in position 2 or 3
CPC
C07D 239/22
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
20having two double bonds between ring members or between ring members and non-ring members
22with hetero atoms directly attached to ring carbon atoms
C07D 239/70
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
C07D 239/90
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
86with hetero atoms directly attached in position 4
88Oxygen atoms
90with acyclic radicals attached in positions 2 or 3
Applicants
  • HOECHST CELANESE CORPORATION [US]/[US]
Inventors
  • BHATTACHARYA, Apurba
  • ALLEN, Diane, E.
Agents
  • FRENKEL,Stuart D.
Priority Data
08/595,88505.02.1996US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR PREPARING PYRIMIDIN DERIVATIVES
(FR) PROCEDE DE PREPARATION DE DERIVES DE PYRIMIDINE
Abstract
(EN)
The present invention provides a process for preparing a 5,6-dihydro-3H-pyrimidin-4-one derivatives which comprises the steps of: (a) dehydrating a N-acyl beta amino acid in the presence of a dehydration agent and an organic solvent for a sufficient period of time and under suitable temperature and pressure conditions to form an oxazone; (b) adding a carboxylic acid and a primary amine salt of a carboxylic acid to said oxazone to form a mixture; (c) distilling azeotropically said mixture for a suitable period of time and under suitable temperature and pressure conditions to substantially remove said dehydration agent and said organic solvent; and (d) heating the product of step (c) for a sufficient period of time and under suitable temperature and pressure conditions to form said pyrimidin derivatives.
(FR)
La présente invention concerne un procédé de préparation de dérivés de 5,6-dihydro-3H-pyrimidin-4-one comprenant les étapes consistant (a) à déshydrater un acide aminé N-acyle$g(b) en présence d'un agent de déshydratation et d'un solvant organique pendant une durée suffisante et dans des conditions de température et de pression appropriées pour former une oxazone, (b) à ajouter un acide carboxylique et un sel d'amine primaire d'un acide carboxylique à ladite oxazone pour former un mélange, (c) à distiller de manière azéotrope ledit mélange pendant une durée suffisante et dans des conditions de température et de pression adaptées afin d'éliminer sensiblement ledit agent de déshydratation ainsi que ledit solvant organique, (d) à chauffer le produit de l'étape (c) pendant une durée suffisante et dans des conditions de température et de pression adaptées pour former lesdits dérivés de pyrimidine.
Also published as
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