61190-11-2Relevant articles and documents
SUBSTITUTED ISOQUINOLINES AND THEIR USE AS TUBULIN POLYMERIZATION INHIBITORS
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Page/Page column 101, (2011/12/14)
The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds
A ONE-POT ISOQUINOLINE SYNTHESIS BY CYCLODEHYDROGENATION OF BENZYLAMINOACETALS WITH CHLOROSULFONIC ACID
Kido, Kazuko,Watanabe, Yasuo
, p. 1151 - 1154 (2007/10/02)
A direct preparation of the fully aromatized isoquinolines (3a-l) by the cyclodehydrogenation of benzylamnoacetals (2a-l) with chlorosulfonic acid is described.Comparing the behavior of chlorosulfonic acid with that of sulfuric acid toward 1,2-dihydroisoquinoline, it is able to be suggested that benzylaminoacetals were cyclized first to 1,2-dihydroisoquinolines, subsequently, dehydrogenated to the fully aromatized isoquinolines by the hydride abstraction with ClSO3H.Subtitution by a larger R3 group than isopropyl in the acetal ArCH(R3)NHCH2CH(OEt)2, interfered this second step, so the corresponding isoquinolines could not be obtained.