Catalytic process for the preparation of thiazole derivatives
There are described a process for the preparation of a compound of formula in free form or in salt form, wherein Q is CH or N; Y is NO 2 or CN; Z is CHR 3 , O, NR 3 or S; R 1 and R 2 are, for example, C 1 -C 8 alkyl or together form an alkylene bridge; R 3 is H or C 1 -C 1-2 alkyl which is unsubstit...
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Main Authors | , , , , |
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Format | Patent |
Language | English |
Published |
12.02.2004
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Online Access | Get full text |
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Abstract | There are described a process for the preparation of a compound of formula in free form or in salt form, wherein Q is CH or N; Y is NO
2
or CN; Z is CHR
3
, O, NR
3
or S; R
1
and R
2
are, for example, C
1
-C
8
alkyl or together form an alkylene bridge; R
3
is H or C
1
-C
1-2
alkyl which is unsubstituted or substituted by R
4
; and R
4
is unsubstituted or substituted aryl or heteroaryl; wherein a) a compound of formula (II), wherein X is a leaving group, is reacted with a chlorinating agent to form a compound of formula (III), in free form or in salt form; and b) the compound of formula (III) thereby obtained is reacted with a compound of formula wherein R
1
, R
2
, Y, Z and Q are as defined for compound (I); in which process the chlorination according to process step a) is performed using a chlorinating agent in the presence of catalytic amounts of SO
2
; a process for the preparation of a compound of formula (III) according to process a) hereinbefore; and the use of the compouds of formulae (II), (III) and (IV) in a process as described hereinbefore.
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AbstractList | There are described a process for the preparation of a compound of formula in free form or in salt form, wherein Q is CH or N; Y is NO
2
or CN; Z is CHR
3
, O, NR
3
or S; R
1
and R
2
are, for example, C
1
-C
8
alkyl or together form an alkylene bridge; R
3
is H or C
1
-C
1-2
alkyl which is unsubstituted or substituted by R
4
; and R
4
is unsubstituted or substituted aryl or heteroaryl; wherein a) a compound of formula (II), wherein X is a leaving group, is reacted with a chlorinating agent to form a compound of formula (III), in free form or in salt form; and b) the compound of formula (III) thereby obtained is reacted with a compound of formula wherein R
1
, R
2
, Y, Z and Q are as defined for compound (I); in which process the chlorination according to process step a) is performed using a chlorinating agent in the presence of catalytic amounts of SO
2
; a process for the preparation of a compound of formula (III) according to process a) hereinbefore; and the use of the compouds of formulae (II), (III) and (IV) in a process as described hereinbefore.
1 |
Author | Desponds, Olivier Gressly, Remy Passafaro, Marco Rapold, Thomas Faber, Dominik |
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Snippet | There are described a process for the preparation of a compound of formula in free form or in salt form, wherein Q is CH or N; Y is NO
2
or CN; Z is CHR
3
, O,... |
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SourceType | Open Access Repository |
Title | Catalytic process for the preparation of thiazole derivatives |
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