61350-65-0Relevant articles and documents
Synthesis and biological evaluation of potential 5-HT7 receptor PET radiotracers
Andries, Julien,Lemoine, Laetitia,Le Bars, Didier,Zimmer, Luc,Billard, Thierry
scheme or table, p. 3455 - 3461 (2011/08/03)
Brain serotonin 7 receptor (5-HT7) is involved in several mood disorders and drug candidates targeting this subtype are currently in development. Positron emission tomography (PET) is a molecular imaging modality offering great promise for accelerating the process from preclinical discovery to clinical phases. As no PET radiopharmaceutical has yet been used successfully to study the 5-HT7 receptor in vivo, our objective is to develop the first 5-HT7 fluorine-18 labeled radiotracer. Four structural analogs of SB269970, a specific 5-HT7 receptor antagonist, divided in FP3 series and FPMP series were synthesized. Their antagonist effects were investigated by cellular functional assay. Nitro-precursors of these analogs were radiolabeled via a [18F-]nucleophilic substitution and in vitro autoradiographies were performed in rat brain. Chemical and radiochemical purities of fluorine radiotracers were >99% with specific activities in 40-129 GBq/μmole range. The four derivates presented antagonism potencies toward 5-HT7 receptors (pKB) between 7.8 and 8.8. The four PET radiotracers had suitable characteristic for 5-HT7 receptor probing in vitro even if the FP3 series seemed to be more specific for this receptor. These results encourage us to pursue in vivo studies.
Asymetric Electrophilic α-Amidoalkylation 4: Generation and Trapping Reactions of Chiral N-Acylpyrrolidiniumions
Wanner, Klaus Th.,Hoefner, Georg
, p. 99 - 103 (2007/10/02)
The pyrrole derivatives 1, 6, and 10 react in the presence of TiCl4 with the silyl enol ether 3 to form α-substituted pyrrolidine amides stereoselectively. 6 and 10 (after HCl-addition =>11) react even at -78 deg C, the reaction of 10 exceeds that of 6 in yield and stereoselctivity.