On October 26, 2012, Woolford, Alison Jo-Anne; Howard, Steven; Buck, Ildiko Maria; Chessari, Gianni; Johnson, Christopher Norbert; Tamanini, Emiliano; Day, James Edward Harvey; Chiarparin, Elisabetta; Heightman, Thomas Daniel; Frederickson, Martyn; Griffiths-Jones, Charlotte Mary published a patent.Electric Literature of 52537-00-5 The title of the patent was Preparation of bicyclic heterocycles as anticancer agents. And the patent contained the following:
The invention relates to bicyclic heterocycles of formula I and tautomeric and stereochem. isomeric forms, N-oxides, pharmaceutically acceptable salts and the solvates thereof as anticancer agents; their preparation and use in the treatment of cancer. Compounds of formula I wherein ring E is a 6-membered aromatic carbocyclyl and heterocyclyl; G and J are independently C and N; Q is CR and N; R1 is (un)substituted C1-4 alkyl, C2-4 alkenyl and C3-8 cycloalkyl; R2 and R4 are independently (un)substituted H, C1-6 alkyl, C2-6 alkenyl, etc.; R2 and R4 together with the carbon attached form 3- to 10-membered saturated carbocyclyl and heterocyclyl; R3 and R10 are independently (un)substituted H, C1-6 alkyl, C2-6 alkenyl, etc.; R2 and R4 together with the carbon attached form 3- to 10-membered saturated carbocyclyl and heterocyclyl; R is (un)substituted C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl, etc.; and tautomeric and stereochem. isomeric forms, N-oxides, pharmaceutically acceptable salts and the solvates thereof, are claimed. Example compound II was prepared by BOC-deprotection of (R)-2-methyl-4-[2-6-methylsulfamoyl-2,3-dihydroindol-1-yl)-2-oxo-ethyl]piperazine-1-carboxylic acid tert-Bu ester. All the invention compounds were evaluated for their antiproliferative activity (some data given). The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Electric Literature of 52537-00-5
The Article related to bicyclic heterocycle preparation anticancer agent, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 52537-00-5
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles