133100-87-5Relevant articles and documents
IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES
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Page/Page column 226, (2010/11/17)
The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+-O- or CR3; Y is N, N+-O- or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
Nature of the Reactions Involving 4-Haloisoquinolines and Amide Ion in Ammonia. Remarkable Competition between SRN1 Substitution and ? Complex Formation
Zoltewicz, John A.,Oestreich, Terence M.
, p. 2805 - 2809 (2007/10/02)
4-Bromo- (1) or 4-chloroisoquinoline (3) in refluxing liquid ammonia containing amide and thiomethoxide reacts preferentially with the thiolate ion to give 4-(methylthio)isoquinoline (2) in high yield.The bromo substrate was shown to require amide ion in order to react with thiomethoxide ion, no reaction taking place in its absence.Substitution product is believed to form from both halides by an SRN1 mechanism.By contrast, 3-chloroisoquinoline under the same conditions of mixed anions gives 3-aminoisoquinoline.The role of amide ion and its addition to give ? complexes in these and other reactions of 4-halogenated isoquinolines in ammonia is discussed.