HPLC of Formula: 399-52-0In 2019 ,《Synthesis of novel pyrido[1,2-c]pyrimidine derivatives with rigidized tryptamine moiety as potential SSRI and 5-HT1A receptor ligands》 appeared in European Journal of Medicinal Chemistry. The author of the article were Slifirski, Grzegorz; Krol, Marek; Kleps, Jerzy; Ulenberg, Szymon; Belka, Mariusz; Baczek, Tomasz; Siwek, Agata; Stachowicz, Katarzyna; Szewczyk, Bernadeta; Nowak, Gabriel; Bojarski, Andrzej; Koziol, Anna E.; Turlo, Jadwiga; Herold, Franciszek. The article conveys some information:
In this study new derivatives of 4-aryl-pyrido[1,2-c]pyrimidine I (R1 = H, Cl, Me, F, OMe; R2 = H, Cl, F, OMe, Me, etc.; R3 = H, F, OMe) having conformationally restricted tryptamine moiety were prepared In vitro studies (RBA) have shown that a few compounds exhibit high affinity to mol. targets 5-HT1A receptor and SERT protein. In general, compounds with an unsubstituted or a para-substituted benzene ring on the pyrido[1,2-c]pyrimidine residue in the terminal part were characterized by higher binding ability, which can be justified by the greater flexibility of the structure. For I [R1 = R2 = R3 = H (II)], I [R1 = H; R2 = F; R3 = H (III)], I (R1 = H; R2 = OMe; R3 = H) and I [R1 = H; R2 = OMe; R3 = OMe (IV)], further in vitro, in vivo and metabolic stability tests were performed. The in vitro studies in the extended receptor profile (D2, 5-HT2A, 5-HT6 and 5-HT7) indicated their selectivity toward the 5-HT1A receptor and SERT protein. The in vivo studies (8-OH-DPAT-induced hypothermia in mice, FST) revealed that II has the properties of presynaptic agonist of the 5-HT1A receptor, and III demonstrated the properties of a presynaptic antagonist of the 5-HT1A receptor. Metabolic stability studies, in turn, showed that few compounds having an unsubstituted indole residue, were more resistant to biotransformation reactions of the first pass phase than was IV containing a 5-methoxy-substituted indole residue. After reading the article, we found that the author used 5-Fluoro-1H-indole(cas: 399-52-0HPLC of Formula: 399-52-0)
5-Fluoro-1H-indole(cas: 399-52-0) is a member of aromaticfluorinated building blocks. Depending on which substituents are present, fluoroaromatic intermediates can be converted into fluorinated or fluorine-free commercial end products.Fluorine-containing aromatics have been incorporated into drugs (hypnotics, tranquilizers, antiinflammatory agents, analgesics, antibacterials).HPLC of Formula: 399-52-0
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