32588-36-6Relevant articles and documents
Rh-Catalyzed C-H bond alkylation of indoles with α,α-difluorovinyl tosylate: Via indolyl group migration
Zhou, Lu,Zhu, Chuan,Loh, Teck-Peng,Feng, Chao
, p. 5618 - 5621 (2018)
Herein we demonstrate that an alkylation of indoles could be accessed through C-H bond functionalization with α,α-difluorovinyl tosylate. The key aspect for the effective alkylation is the influence of the fluorine substituents on the reactivity of the CC double bond, allowing regioselective insertion as well as an indolyl group shift process. Furthermore, the fluorides are removed through alcoholysis to furnish the alkylation product as a traceless auxiliary.
Design of selective peptidomimetic agonists for the human orphan receptor BRS-3
Weber, Dirk,Berger, Claudia,Eickelmann, Peter,Antel, Jochen,Kessler, Horst
, p. 1918 - 1930 (2007/10/03)
New tool substances may help to unravel the physiological role of the human orphan receptor BRS-3 and its possible use as a drug target for the treatment of obesity and cancer. In continuation of our work on BRS-3, the solid- and solution-phase synthesis of a library of low molecular weight peptidomimetic agonists based on the recently developed short peptide agonist 4 is described. Functional potencies of the compounds were determined measuring calcium mobilization in a fluorometric imaging plate reader (FLIPR) assay. Focusing on the N-terminus, the D-Phe-Gln moiety of 4 was modified in a combinatorial SAR-oriented medicinal chemistry approach. With the incorporation of N-arylated glycine and alanine building blocks azaglycine, piperazine, or piperidine and the synthesis of semicarbazides and semicarbazones, a number of highly potent and selective compounds with a reduced number of peptide bonds were obtained, which also should have enhanced metabolic stability.
INDOLE DERIVATIVES AS DOPAMINE D4 ANTAGONISTS
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, (2008/06/13)
Compound of formula (I), or a pharmaceutically acceptable salt thereof or a prodrug thereof wherein E represents--CH 2--or--CH. sub.2 CH. sub. 2--; R represents hydrogen or C 1-6 alkyl; Q represents a moiety of formula Qa, Qb, Qc or Qd which are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D. sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs. STR1
