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1. (WO2011029762) PROCESS FOR PREPARING ALPHA-CARBOXAMIDE DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2011/029762 International Application No.: PCT/EP2010/062826
Publication Date: 17.03.2011 International Filing Date: 01.09.2010
IPC:
C07D 207/16 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
04
having no double bonds between ring members or between ring members and non-ring members
10
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
16
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Applicants:
ZAJAC, Matthew, Allen [US/US]; US (UsOnly)
CONVERGENCE PHARMACEUTICALS LIMITED [GB/GB]; 90, High Holborn London, WC1V 6XX, GB (AllExceptUS)
Inventors:
ZAJAC, Matthew, Allen; US
Agent:
GIBSON, Mark; Sagittarius IP Taylor House 39, High Street Marlow, Bucks SL7 1 AF, GB
Priority Data:
61/242,00314.09.2009US
Title (EN) PROCESS FOR PREPARING ALPHA-CARBOXAMIDE DERIVATIVES
(FR) PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS ALPHA-CARBOXAMIDES
Abstract:
(EN) The present application provides a process for the preparation of α-carboxamide pyrrolidine derivatives of formula (I), wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or such R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R5 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; either R6 or R7 is -O-R8, -OCHR9R8, -NCH2R8 or -(CH2)2R8 wherein the other R6 or R7 is hydrogen or R5; and wherein R8 is a phenyl ring or wherein the phenyl ring is optionally substituted by one or more groups independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; and R9 is hydrogen or C1-3alkyl.
(FR) La présente invention porte sur un procédé pour la préparation de dérivés α-carboxamides de pyrrolidine de formule (I), dans laquelle R1 et R2 représentent chacun indépendamment hydrogène, alkyle en C1-6 ou (cycloalkyl en C3-6)(alkyle en C1-6) ; ou de tels R1 et R2, conjointement avec l'azote auquel ils sont attachés, peuvent former un noyau saturé de 3, 4, 5 ou 6 chaînons non substitué ; X représente le carbone ou l'azote ; n vaut 0, 1 ou 2 ; le cas échéant chaque R5 est indépendamment choisi dans la liste constituée par alkyle en C1-3, halogène, cyano, haloalkyle en C1-3, hydroxy, alcoxy en C1-3 et haloalcoxy en C1-3 ; l'un ou l'autre de R6 ou R7 représente -O-R8, -OCHR9R8, -NCH2R8 ou -(CH2)2R8, l'autre de R6 ou R7 représentant l'hydrogène ou R5 ; et R8 représentant un noyau phényle ou le noyau phényle étant éventuellement substitué par un ou plusieurs groupes indépendamment choisis dans la liste constituée par alkyle en C1-3, halogène, cyano, haloalkyle en C1-3, hydroxy, alcoxy en C1-3 et haloalcoxy en C1-3 ; et R9 représente hydrogène ou alkyle en C1-3.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, 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, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, 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, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, 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, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)