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1. (WO2013162764) METHODS FOR THE SYNTHESIS OF ETHYLFUMARATES AND THEIR USE AS INTERMEDIATES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2013/162764 International Application No.: PCT/US2013/032162
Publication Date: 31.10.2013 International Filing Date: 15.03.2013
IPC:
C07D 241/08 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
241
Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
02
not condensed with other rings
06
having one or two double bonds between ring members or between ring members and non-ring members
08
with oxygen atoms directly attached to ring carbon atoms
Applicants: MANNKIND CORP[US/US]; 1 Casper St Danbury, CT 06810, US
Inventors: KRAFT, Kelly; US
FREEMAN, John; US
SERWINSKI, Paul; US
PAVIA, Vinnie; US
PHANTSIEL, Otto; US
KAUR, Navneet; US
Agent: JACKSON, Christopher; 1100 Fifth Third Center 21 East State St. Columbus, OH 43215, US
Priority Data:
61/639,53627.04.2012US
Title (EN) METHODS FOR THE SYNTHESIS OF ETHYLFUMARATES AND THEIR USE AS INTERMEDIATES
(FR) PROCÉDÉS DE SYNTHÈSE DE FUMARATES D'ÉTHYLE ET LEUR UTILISATION EN TANT QU'INTERMÉDIAIRES
Abstract:
(EN) Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.
(FR) L'invention concerne des modes de réalisation relatifs à des procédés de synthèse améliorés d'intermédiaires de fumarate activés et leur utilisation dans une synthèse chimique. Des modes de réalisation selon l'invention décrivent la synthèse d'esters de fumarate activés comprenant ceux dérivés de groupes d'activation comprenant : le 4-nitrophényle, l'azoture de diphénylphosphoryle, le chlorure de pivaloyle, l'isocyanate de chlorosulfonyle, le p-nitrophénol, le MEF, le trifluoroacétyle et le chlore, par exemple, le chlorure d'éthylfumaroyle et l'utilisation consécutive de l'ester activé in situ. D'autres modes de réalisation décrivent la synthèse améliorée d'aminoalkyldicétopipérazines à partir d'intermédiaires non isolés et non purifiés permettant des rendements et un débit de réacteur améliorés.
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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, 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, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, 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, 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, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)