Reactions of triphenylphosphine with 2,3-dihalo-2-methylpropionic acids and their methyl esters
摘要:
Triphenylphosphine reacts with 2,3-dichloro-2-methylpropionic acid and its ester along the dehydrochlorination pathway with the participation of the less labile hydrogen atom from the methyl group. The subsequent reaction of the unsaturated product with triphenylphosphine yields 2-carboxypropane- and 2-methoxycarbonylpropane-1,3-diylbis(triphenylphosphonium) dichlorides, respectively. The unusual course of dehydrochlorination may be due to easier electron density transfer from the C-H bond of the methyl group as compared to the chloromethyl group in the carbocationoid intermediate. With the bromine analogs, the reaction pathways are different. The ester reacts similarly to dibromopropionic acid and its derivatives, following the debromination scheme, whereas the free acid gives the product of double nucleophilic substitution.
Novel substituted indolines with an inhibitory effect on various kinases and complexes of CDKs
申请人:Boehringer Ingelheim Pharma KG
公开号:US20040058978A1
公开(公告)日:2004-03-25
The present invention relates to new substituted indolinones of general formula
1
wherein
X and R
1
to R
5
are defined as in claim 1, the isomers and the salts thereof which have valuable properties.
The above compounds of general formula I wherein R
1
denotes a hydrogen atom, a C
1-3
-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R
1
does not represent a hydrogen atom, a C
1-3
-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.
NEUE SUBSTITUIERTE INDOLINONE MIT EINER INHIBIERENDEN WIRKUNG AUF VERSCHIEDENE KINASEN UND CYCLIN/CDK-KOMPLEXE
申请人:Boehringer Ingelheim Pharma GmbH & Co.KG
公开号:EP1115704B1
公开(公告)日:2003-06-18
US6855710B2
申请人:——
公开号:US6855710B2
公开(公告)日:2005-02-15
US6921767B2
申请人:——
公开号:US6921767B2
公开(公告)日:2005-07-26
[EN] NOVEL PROCESSES FOR THE SYNTHESIS OF CYCLOPROPYL COMPOUNDS<br/>[FR] NOUVEAUX PROCESSUS DE SYNTHESE DE COMPOSES DE CYCLOPROPYLE
申请人:PHARMACIA CORP
公开号:WO2005051904A2
公开(公告)日:2005-06-09
This invention relates to processes for the preparation of cyclopropyl compounds of Formula: (I) wherein: x is an integer selected from the group consisting of 0, 1 and 2; R1 and R2 are independently selected from the group consisting of H, C1-C6 alkyl, and halo; and R3, R4, R5, R6 and R7 are independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, and halo.