WIPO logo
Mobile | Deutsch | Español | Français | 日本語 | 한국어 | Português | Русский | 中文 | العربية |
PATENTSCOPE

Search International and National Patent Collections
World Intellectual Property Organization
Search
 
Browse
 
Translate
 
Options
 
News
 
Login
 
Help
 
Machine translation
1. (WO2015126860) PROCESS FOR PREPARING N-BENZYL-3-HYDROXY-4-SUBSTITUTED-PYRIDIN-2-(1H)-ONES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2015/126860    International Application No.:    PCT/US2015/016243
Publication Date: 27.08.2015 International Filing Date: 18.02.2015
IPC:
A61K 31/497 (2006.01), C07D 401/06 (2006.01)
Applicants: AERPIO THERAPEUTICS, INC. [US/US]; 9987 Carver Road Suite 420 Cincinnati, OH 45242 (US)
Inventors: ALBERICO, Dino; (CA).
DIXON, Craig; (CA).
GORIN, Boris; (CA).
OUDENES, Jan; (CA)
Agent: ECHLER, Richard, S.; (US)
Priority Data:
61/941,540 19.02.2014 US
Title (EN) PROCESS FOR PREPARING N-BENZYL-3-HYDROXY-4-SUBSTITUTED-PYRIDIN-2-(1H)-ONES
(FR) PROCÉDÉ DE PRÉPARATION DE N-BENZYL-3-HYDROXY-4-SUBSTITUÉ-PYRIDINE-2-(1H)-ONES
Abstract: front page image
(EN)Disclosed herein is a process for preparing N-benzyl-3-hydroxypyridin-2-(1H)-ones that are substituted at the pyridine ring 4-position with a 4-carbamoylpiperazin-1-yl moiety. The process comprises A) reacting 3-hydroxypyridin-2(1 H)-one with a benzylating agent in the presence of a silylating reagent that provides at least 2 equivalents of a silyl protecting group and a proton source; to form a N-benzyl-3-hydroxypyridin-2(1 H)-one; and B) reacting the N-benzyl-3-hydroxypyridin-2(1 H)-one formed in Step (A) with a carbamoylpiperazine, in the presence of a source of formaldehyde and an acid to form the substituted N-benzyl-3-hydroxypyridin-2-(1 H)-one.
(FR)L'invention concerne un procédé de préparation de N-benzyl-3-hydroxypyridine-2-(1H)-ones qui sont substitués au niveau de la position 4 du noyau pyridine par une fraction 4-carbamoylpipérazine-1-yl. Le procédé consiste à: A) faire réagir 3-hydroxypyridine-2(1H)-one avec un agent de benzylation en présence d'un réactif de silylation qui fournit au moins 2 équivalents d'un groupe de protection silyle et une source de protons; former un N-benzyl -3-hydroxypyridine-2(1H)-one; et B) faire réagir le N-benzyl-3-hydroxypyridine-2(1 H)-one formé à l'étape (A) avec une carbamoylpipérazine, en présence d'une source de formaldéhyde et d'un acide pour former N-benzyl-3-hydroxypyridine-2-(1 H)-one substitué.
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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)