On September 24, 2009, Foulon, Loiec; Goullieux, Laurent; Pouzet,brigitte; Serradeil-Le Gal, Claudine; Valette, Gerard published a patent.Recommanded Product: 872046-08-7 The title of the patent was Preparation of 3-aminoalkyl-1,3-dihydro-2H-indol-2-one derivatives as selective V1a arginine vasopressin receptor ligands and in some cases as V1b ligands as well. And the patent contained the following:
The invention is related to the preparation of 3-aminoalkylindolin-2-one derivatives I [X = C1-5 alkylene optionally substituted at ≥1 C atoms by 1 F or by a C1-3 alkyl; R1 = NR8R9, (un)substituted piperidin-4-yl, piperidin-3-yl; R8, R9 = independently H, alkyl; or NR8R9 = heterocyclyl selected from azetidin-4-yl, pyrrolidin-4-yl, morpholin-4-yl, piperazin-4-yl, etc., the C atoms being optionally substituted by ≥1 F atoms; R2 = halo, Alk, OAlk; Alk = = alkyl optionally substituted by ≥1 F atoms; R3 = OMe; R4, R7 = independently H, halo, OH, Alk, OAlk; R5 = H, CO2Alk, CH2OH, R4; R6 = H, OH, Alk, OAlk, cycloalkyloxy, NHCONH2 and derivatives; or R7 is in the 3-position of the Ph group and together with R6 they represent a CH2CH2CH2 radical] their acid addition salts and their hydrates or solvates, having a strong affinity and high selectivity for human V1a arginine vasopressin receptors and in some cases also a strong affinity for V1b receptors. Thus, a multi-step synthesis from 1-chloro-5-fluoro-2-methoxy-4-nitrobenzene and Me 2-(2-fluorophenyl)acetate was given for indolinone (+)-II·×HCl. In an in vitro assay, II bound selectively to human V1a receptor with IC50 = 2.4 nM compared to human V1b, human V2 vasopressin receptors and human oxytocin receptor (Ic50 = >1000 nM, 450 nM and 390 nM, resp.). The V1a antagonistic activity of II was determined in vitro in a FLIPR test measuring the intracellular calcium in cells expressing the human V1a receptors. The experimental process involved the reaction of Methyl 2-(2,6-difluorophenyl)acetate(cas: 872046-08-7).Recommanded Product: 872046-08-7
The Article related to indolinone aminoalkyl preparation selective v2 vasopressin antagonist, vasopressin v2 receptor ligand aminoalkyldihydrohindolone preparation, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Recommanded Product: 872046-08-7
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics