223760-99-4Relevant academic research and scientific papers
PROCESSES FOR THE PREPARATION OF N-HETEROARYL-N-ARYL-AMINES BY REACTING AN N-ARYL CARBAMIC ACID ESTER WITH A HALO-HETEROARYL AND ANALOGOUS PROCESSES
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Page 41, (2010/02/08)
The present invention relates to processes for producing a diaryl amine compound of the formula (I); or a salt thereof, said process comprising the step of coupling a compound of formula (II) with an amine of formula (III) in the presence of an alkali metal salt or a transition metal catalyst, wherein: Ar1 and Ar2 are independently Q; wherein each Q is an aryl or heteroaryl ring system optionally fused to a saturated or unsaturated 5-8 membered ring having 0-4 heteroatoms; wherein Q is optionally substituted as defined in claim 1, wherein: X is a leaving group; and Y is -C(O)-O-Z; and Z is selected from C1-C6 aliphatic, benzyl, Fmoc, -SO2R’ and Q, provided that Q is not substituted with X or alkyne; wherein R’ is as defined in claim 1.
Imidazole derivatives and their use as farnesyl protein transferase inhibitors
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Page column 52, (2010/11/29)
The present invention relates to compounds of formula (I), wherein Ar1represents (A) and (B) or (C); R12and R13are independently hydrogen or C1-4alkyl; Ar2is phenyl or heteroaryl; p is 0 or 1; Ar3is phenyl, pyridinyl, pyridazinyl, pyrimidyl or pyrazynyl, the ring being substituted on ring carbon atoms by R2and —(CH2)nR3, and wherein Ar3is attached to Ar1C(R12)R13CH(Ar2)O— by a ring carbon atom; R2is a group of formula (2), or R2represents a lactone of formula (3), the group of formula (2) or (3) havingLorDconfiguration at the chiral alpha carbon in the corresponding free amino acid; n is 0, 1 or 2; R3is phenyl or heteroaryl; and R5-R9, m and n are as defined in the specification; or a pharmaceutically acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use in cancer therapy.
