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1. (WO1997018190) N-PROTECTED/N-SUBSTITUTED-BETA-AMINO HYDROXY SULFONATES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018190 International Application No.: PCT/US1996/018177
Publication Date: 22.05.1997 International Filing Date: 08.11.1996
Chapter 2 Demand Filed: 12.06.1997
IPC:
C07C 221/00 (2006.01) ,C07C 309/14 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
221
Preparation of compounds containing amino groups and doubly-bound oxygen atoms bound to the same carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
309
Sulfonic acids; Halides, esters, or anhydrides thereof
01
Sulfonic acids
02
having sulfo groups bound to acyclic carbon atoms
03
of an acyclic saturated carbon skeleton
13
containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
14
containing amino groups bound to the carbon skeleton
Applicants:
G.D. SEARLE & CO. [US/US]; Corporate Patent Dept. P.O. Box 5110 Chicago, IL 60680-5110, US (AllExceptUS)
WIECZOREK, Joseph, J. [US/US]; US (UsOnly)
Inventors:
WIECZOREK, Joseph, J.; US
Agent:
KEANE, J., Timothy ; G.D. Searle & Co. Corporate Patent Dept. P.O. Box 5110 Chicago, IL 60680-5110, US
BEIL, Hans, Chr.; Adelonstrasse 58 Postfach 80 01 40 D-65901 Frankfurt am Main, DE
Priority Data:
60/006,86016.11.1995US
Title (EN) N-PROTECTED/N-SUBSTITUTED-BETA-AMINO HYDROXY SULFONATES
(FR) BETA-AMINO HYDROXYSULFONATES N PROTEGES/SUBSTITUES
Abstract:
(EN) N-Protected/N-substituted alpha-amino aldehydes, which are useful as pharmaceuticals and pharmaceutical intermediates, can be stored and shipped in a more stable form as N-protected/N-substituted-beta-amino hydroxy sulfonates of formula ($g(a)), wherein W represents a cation which is capable of forming a sulfonate salt; R1 represents alkyl, alkenyl, alkyl substituted with one or more aryl radicals, cycloalkenylalkyl, alkanoyl, haloalkanoyl, aroyl, alkoxycarbonyl, aralkoxycarbonyl, heteroaralkoxycarbonyl or 9-phenylfluoren-9-yl radicals; R2 represents hydrogen, alkyl, alkenyl, aralkyl, cycloalkyl, cycloalkenylalkyl or aryl radicals; or NR1R2 represents heterocyclo or heteroaryl radicals; and R3 represents alkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, aryloxyalkyl, alkylthioalkyl, arylthioalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl or cycloalkylalkyl radicals; or R2 and R3 together with the nitrogen and the carbon atom to which they are bonded form a heterocyclo radical; which can be readily converted back into the aldehyde under mild conditions. The present invention relates to N-protected/N-substituted-beta-amino hydroxy sulfonates and their use.
(FR) Des alpha-amino aldéhydes N protégés/substitués, qui sont utiles comme produits pharmaceutiques et comme intermédiaires pour des produits pharmaceutiques, peuvent être conservés et transportés sous une forme plus stable de bêta-amino hydroxysulfonates N protégés/substitués, ayant la formule ($g(a)). Dans cette formule, W représente un cation qui est capable de former un sel de sulfonate; R1 représente des radicaux alkyle, alcényle, alkyle substitué avec un ou plusieurs radicaux aryle, cycloalcénylalkyle, alcanoyle, haloalcanoyle, aroyle, alcoxycarbonyle, aralcoxycarbonyle, hétéroaralcoxycarbonyle ou 9-phénylfluorèn-9-yle; R2 représente des radicaux hydrogène, alkyle, alcényle, aralkyle, cycloalkyle, cycloalcénylalkyle ou aryle; ou NR1R2 représente des radicaux hétérocyclo ou hétéroaryle; et R3 représente des radicaux alkyle, haloalkyle, cyanoalkyle, hydroxyalkyle, alcoxyalkyle, aryloxyalkyle, alkylthioalkyle, arylthioalkyle, aryle, aralkyle, hétéroaryle, hétéroaralalkyle, cycloalkyle ou cycloalkylalkyle; ou R2 et R3 forment un radical hétérocyclo avec l'atome d'azote et l'atome de carbone auxquels ils sont fixés. Ces composés peuvent être facilement reconvertis en aldéhyde correspondant, dans des conditions douces. L'invention concerne également ces bêta-amino hydroxysulfonates N protégés/substitués et leur utilisation.
Designated States: AL, AM, AT, AU, AZ, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0861233JP3974656 JP2000500459 CA2237936AU1997012718