On January 12, 2012, Nakamura, Tsuyoshi; Namiki, Hidenori; Terasaka, Naoki; Shima, Akiko; Hagihara, Masahiko; Iwase, Noriaki; Takata, Katsunori; Kikuchi, Osamu; Tsuboike, Kazunari; Setoguchi, Hiroyuki; Yoneda, Kenji; Sunamoto, Hidetoshi; Ito, Koji published a patent.Formula: C7H9ClN2 The title of the patent was Preparation of tetrahydroquinoline compounds as CETP inhibitors. And the patent contained the following:
Title compounds I [R1 = H, alkyl, hydroxyalkyl, etc.; or pharmacol. acceptable salts thereof], useful for the treatment of dyslipidemia, hypercholesterolemia, arteriosclerosis, etc., were prepared For example, conversion of 4,4-difluorocyclohexanecarboxylic acid Et ester into II [PMB = p-methoxybenzyl] in a multi-step process followed by treatment with 4-CF3PhMgBr, diastereomeric separation, fluorination, de-alkoxycarbonylation, chiral separation, reaction with 2-bromopyrimidine, and debenzylation afforded compound III [R = pyrimidin-2-yl]. In CETP (cholesteryl ester transfer protein) inhibition assays, IC50 of III [R = 5-(4-methylpiperazin-1-yl)pyrimdin-2-yl] was 19 nM. Pharmaceutical formulations containing I are disclosed. The experimental process involved the reaction of 2-Chloro-5-isopropylpyrimidine(cas: 596114-50-0).Formula: C7H9ClN2
The Article related to tetrahydroquinoline preparation cetp inhibitor, dyslipidemia hypercholesterolemia arteriosclerosis treatment tetrahydroquinoline cetp inhibition, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C7H9ClN2
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia