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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)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965
Non-condensed pyrazines
497
containing further heterocyclic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
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:
61/941,54019.02.2014US
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:
(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 (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)