854534-81-9Relevant academic research and scientific papers
Practical synthesis of precursor of [N-methyl-11C]vorozole, an efficient PET tracer targeting aromatase in the brain
Takahashi, Kayo,Yamagishi, Gen,Hiramatsu, Toshiyuki,Hosoya, Ayako,Onoe, Kayo,Doi, Hisashi,Nagata, Hiroko,Wada, Yasuhiro,Onoe, Hirotaka,Watanabe, Yasuyoshi,Hosoya, Takamitsu
, p. 1464 - 1470 (2011/04/12)
A practical method to prepare precursor of [N-methyl-11C] vorozole ([11C]vorozole), an efficient positron emission tomography (PET) tracer for imaging aromatase in the living body, was established. Sufficient amount of the racemate including norvorozole, a demethylated vorozole derivative used as a precursor of [11C]vorozole, became available by means of high-yield eight-step synthesis. The enantiomers were separated by preparative HPLC using a chiral stationary phase column to give optically pure norvorozole and its enantiomer. From the latter, ent-[11C]vorozole, an enantiomer of [11C]vorozole, was prepared and used in the PET study for the first time, which was shown to bind very weakly to aromatase in rhesus monkey brain supporting the previous pharmacological results. The stable supply of norvorozole will facilitate further researches on aromatase in the living body including brain by the PET technique.
6-ALKENYL AND 6-PHENYLALKYL SUBSTITUTED 2-QUINOLINONES AND 2-QUINOXALINONES AS POLY(ADP-RIBOSE) POLYMERASE INHIBITORS
-
Page/Page column 51, (2010/02/12)
The present invention provides compounds of formula (I) and compounds of formula (I), (VII-a), as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.
