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1. (WO2017036432) A PRODUCTION METHOD OF 1-(4-FLUOROBENZYL)-3-(4-ISOBUTOXYBENZYL)-1-(1-METHYLPIPERIDIN- 4— YL)UREA AND ITS DEUTERATED ANALOGS NOT CONTAINING DIMERIC IMPURITIES
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Pub. No.: WO/2017/036432 International Application No.: PCT/CZ2016/000093
Publication Date: 09.03.2017 International Filing Date: 18.08.2016
IPC:
C07D 211/58 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
211
Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
04
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
06
having no double bonds between ring members or between ring members and non-ring members
36
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
56
Nitrogen atoms
58
attached in position 4
Applicants:
ZENTIVA, K.S. [CZ/CZ]; U Kabelovny 130 102 37 Praha 10, CZ
Inventors:
RADL, Stanislav; CZ
STACH, Jan; CZ
KLECAN, Ondrej; CZ
Agent:
JIROTKOVA, Ivana; ROTT, RUZICKA & GUTTMANN Vinohradska 37, 120 00 Praha 2, CZ
Priority Data:
PV 2015-60102.09.2015CZ
Title (EN) A PRODUCTION METHOD OF 1-(4-FLUOROBENZYL)-3-(4-ISOBUTOXYBENZYL)-1-(1-METHYLPIPERIDIN- 4— YL)UREA AND ITS DEUTERATED ANALOGS NOT CONTAINING DIMERIC IMPURITIES
(FR) PROCÉDÉ DE PRODUCTION DE 1-(4-FLUOROBENZYL)-3-(4-ISOBUTOXYBENZYL)-1-(1-MÉTHYLPIPÉRIDIN-4-YL)URÉE ET DE SES ANALOGUES DEUTÉRÉS NE CONTENANT PAS D’IMPURETÉS SOUS FORME DE DIMÈRES
Abstract:
(EN) The invention relates to an improved production method of 1-(4-fluorobenzyl)-3-(4-- isobutoxybenzyl)-1-(1— methylpiperidin-4-yl)urea of formula I, known under the generic name of pimavanserin. The method consists of two steps, namely a reaction of N-(4- fluorobenzyl)-l-methylpiperidine-4-amine with cyanic acid, the next step being a reaction of the obtained compound from the first step, 1-(4-fluorobenzyl)-1-(1-methylpiperidin-4-yl)urea and 4-isobutoxybenzaldehyde or with its precursors. Pimavanserin is an inverse agonist of the serotonin 5-HT2A receptor and is currently in the tartrate form in stage III of clinical trial for the treatment of psychosis in patients suffering from Parkinson's disease and has potential to become part of the therapy of other psychotic conditions.
(FR) L'invention concerne un procédé de production amélioré de 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-méthylpipéridin-4-yl)urée de formule I, connue sous le nom générique de pimavansérine. Le procédé comporte deux étapes, à savoir une réaction entre de la N-(4-fluorobenzyl)-1-méthylpipéridine-4-amine et de l'acide cyanique, l'étape suivante étant une réaction entre le composé obtenu à la première étape, de la 1-(4-fluorobenzyl)-1-(1-méthylpipéridin-4-yl)urée et du 4-isobutoxybenzaldéhyde ou ses précurseurs. La pimavansérine est un agoniste inverse du récepteur de la sérotonine 5-HT2A et se trouve actuellement sous forme de tartrate en phase III d'un essai clinique sur le traitement de la psychose chez des patients souffrant de la maladie de Parkinson et pourrait potentiellement faire partie intégrante de la thérapie contre d'autres troubles psychotiques.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)