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1. (WO2017205539) DIAZENE DIRECTED MODULAR SYNTHESIS OF COMPOUNDS WITH QUATERNARY CARBON CENTERS
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Pub. No.: WO/2017/205539 International Application No.: PCT/US2017/034327
Publication Date: 30.11.2017 International Filing Date: 24.05.2017
IPC:
A61K 31/407 (2006.01) ,C07D 209/40 (2006.01) ,C07D 487/04 (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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
407
condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
30
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
40
Nitrogen atoms, not forming part of a nitro radical, e.g. isatin semicarbazone
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY[US/US]; 77 Massachusetts Ave Cambridge, Massachusetts 02139, US
Inventors: MOVASSAGHI, Mohammad; US
LINDOVSKA, Petra; US
Agent: ZHANG, Wei; US
Priority Data:
62/340,94824.05.2016US
Title (EN) DIAZENE DIRECTED MODULAR SYNTHESIS OF COMPOUNDS WITH QUATERNARY CARBON CENTERS
(FR) SYNTHÈSE MODULAIRE DIRIGÉE PAR DIAZÈNE DE COMPOSÉS À CENTRES DE CARBONE QUATERNAIRE
Abstract:
(EN) Diazene-directed modular synthesis is described for the preparation Csp2-Csp3 and Csp3-Csp3 linkages where one or more stereogenic quaternary carbon centers are formed. The disclosed methods are directed to the preparation of compounds of Formula (I), or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, from compounds of Formula (II) wherein R1-R5 and q are as defined independently for each occurrence herein. A wide variety of compounds can be accessed in this manner, including oligocyclotryptamines, where the stereochemistry of each subunit is beneficially secured before fragment coupling.
(FR) La présente invention concerne une synthèse modulaire dirigée par diazène destinée à la préparation de liaisons Csp2-Csp3 et Csp3-Csp3, où un ou plusieurs centres de carbone quaternaire stéréogènes sont formés. Les procédés décrits concernent la préparation de composés de formule (I), ou d'un sel, d'un tautomère ou d'un stéréoisomère de qualité pharmaceutique de ces derniers, à partir de composés de formule (II) : dans laquelle R1 à R5 et q sont tels que définis indépendamment, pour chaque occurrence, dans la description. On peut accéder à une grande variété de composés de cette manière, y compris des oligocyclotryptamines, la stéréochimie de chaque sous-unité étant avantageusement fixée avant le couplage des fragments.
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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, DJ, 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, KH, KN, KP, KR, KW, 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)