Novel triazolo pyrimidine compounds
AssigneeAstraZeneca AB
InventorsUlf Larsson, Mattias Magnusson, Tibor Musil, Andreas Palmgren
Life of this patent
Estimating the term…
Abstract
The present invention relates to a pyrimidine compound (I) useful as a pharmaceutical intermediate, to a process for preparing said pyrimidine compound, to intermediates used in said process, and to the use of said pyrimidine compound in the preparation of pharmaceuticals.
Claims9
A compound of formula (I):
- 21
A process for preparing a compound of formula (I), comprising reacting a compound of formula (II):
- 22
- with a salt of a compound of formula (III):
- 23
A process for preparing a compound of formula (II):
- 25
- comprising hydrogenating a compound of formula (IV):
- 26
- wherein Ar is phenyl optionally substituted by halogen, C1-4 alkyl or C1-4 alkoxy.
The use of a compound of formula (I) to prepare a compound of formula (A):
- 28
- comprising:
- (a) reacting a compound of formula (I) with an alkali metal nitrite in the presence of a suitable acid to prepare a compound of formula (VII):
- 29
- (b) coupling the compound of formula (VII) with a compound of formula (VI):
- 30
- to provide a compound of formula (V):
- 31
- and,
- (c) deprotecting a compound of formula (V) to provide the compound of formula (A).
A process for preparing a salt of a compound of formula (III):
- 32
- comprising reacting a compound of formula (III) with the necessary acid.
A process for preparing a salt of a compound of formula (III):
- 33
- comprising the steps:
- (a) preparing a compound of formula (XI):
- 34
- by reacting a compound of formula (XII):
- 35
- with benzyl chloroformate;
- (b) preparing a compound of formula (X):
- 36
- by reacting a compound of formula (XI) with a compound L-CH2CO2R* {wherein R* is C1-4 alkyl;
- and L is a leaving group};
- (c) preparing a compound of formula (IX):
- 37
- by reducing a compound of formula (X);
- (d) preparing a compound of formula (III):
- 38
- by deprotecting a compound of formula (IX);
- and,
- (e) preparing a salt of a compound of formula (III) by reacting the compound of formula (III) with the necessary acid.
An intermediate compound of formula (II), (IV), (VII), (VIII), (X) or (XI) or a salt of a compound of formula (III).
Dependencies are inferred from the claim text.