On November 28, 2013, Hamaguchi, Wataru; Kinoyama, Isao; Koganemaru, Yohei; Miyazaki, Takehiro; Kaneko, Osamu; Sekioka, Ryuichi; Washio, Takuya published a patent.COA of Formula: C9H8F2O2 The title of the patent was Preparation of tetrahydroisoquinoline derivatives as modulators of serotonin 5-HT5A receptor for treating dementia and schizophrenia. And the patent contained the following:
To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HT5A receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HT5A receptor regulating action and an excellent pharmacol. action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed. Compounds of formula I [R1 = H, (un)substituted O-alkyl, O-(halogeno-alkyl), or aryl, heteroaryl, cycloalkyl, or cycloalkenyl; R2 = H, alkyl, halogeno-alkyl, halogen, CN, OH, O-alkyl, O-(halogeno-alkyl), alkylene-OH, alkylene-O-alkyl, or cycloalkyl; L = C(R3)(R4)-(CH2)n; R3 and R4 independently = H, alkyl, halogen, OH, or O-alkyl; m = 1-2; n = 0-2], and their pharmaceutically acceptable salts, are prepared Thus, e.g., II was prepared by reaction of 8-(5-chloro-3-fluoropyridin-2-yl)-5-fluoro-1,2,3,4-tetrahydroisoquinoline hydrochloride with DMF. Compounds of the invention were tested for their human 5-HT5A receptor binding inhibition activity, e.g., II showed Ki value of 4.3 nM. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).COA of Formula: C9H8F2O2
The Article related to tetrahydroisoquinoline preparation serotonin 5ht5a receptor dementia schizophrenia, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.COA of Formula: C9H8F2O2
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