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1. (WO2000063186) PROCESS AND INTERMEDIATES FOR PREPARING BENZODIAZEPINES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2000/063186    International Application No.:    PCT/EP2000/003260
Publication Date: 26.10.2000 International Filing Date: 12.04.2000
Chapter 2 Demand Filed:    10.10.2000    
IPC:
C07C 217/58 (2006.01), C07C 225/12 (2006.01), C07C 237/08 (2006.01), C07D 243/14 (2006.01), C07D 401/14 (2006.01)
Applicants: SMITHKLINE BEECHAM PLC [GB/GB]; New Horizons Court, Brentford, Middlesex TW8 9EP (GB) (For All Designated States Except US).
HAYES, Jerome, Francis [GB/GB]; (GB) (For US Only)
Inventors: HAYES, Jerome, Francis; (GB)
Agent: VALENTINE, Jill, Barbara; SmithKline Beecham, Corporate Intellectual Property, Two New Horizons Court, Brentford, Middlesex TW8 9EP (GB)
Priority Data:
9908662.1 15.04.1999 GB
Title (EN) PROCESS AND INTERMEDIATES FOR PREPARING BENZODIAZEPINES
(FR) PROCEDE ET INTERMEDIAIRES DE PREPARATION DES BENZODIAZEPINES
Abstract: front page image
(EN)A new process and intermediates for preparing 1,4-benzodiazepines of formula (I) is disclosed: wherein, R?1¿ is H, OH, Br, I, NR?5¿R?6¿, CO¿2?R?7¿, CF¿3?SO¿3?, C¿1-4?alkoxy, or (4,4'-bipiperidinyl) carbonyl; R?2¿ is alkyl, optionally substituted by CO¿2?R?7¿ or CONR?5¿R?6¿; R?3¿ and R?3'¿ are independently H, Ar or C¿1-6? alkyl optionally substituted by OH, NO¿2?, NH¿2?, NR?5¿R?6¿, halogen, CO¿2?R?7¿, CONR?5¿R?6¿ or Ar, or together R?3¿ and R?3'¿ are =O; R?4¿ is H or C¿1-4? alkyl, optionally substituted by OH, NO¿2?, NH¿2?, NR?5¿R?6¿, halogen, CO¿2?R?7¿, CONR?5¿R?6¿, or Ar; R?5¿ and R?6¿ are independently H, Ar, C¿1-6?alkyl, HCO, C¿1-6?alkyl-CO, Ar-CO, C¿1-6?alkyl-SO¿2?, or Ar-SO¿2?; and R?7¿ is a carboxylic acid protecting group.
(FR)Cette invention se rapporte à un nouveau procédé et à de nouveaux intermédiaires servant à la préparation des 1,4-benzodiazépines représentées par la formule (I), où R?1¿ représente H, OH, Br, I, NR?5¿R?6¿, CO¿2?R?7¿, CF¿3?SO¿3?, alcoxy C¿1-4?, ou (4,4'-bipipéridinyl)carbonyle; R?2¿ représente alkyle, éventuellement substitué par CO¿2?R?7¿ ou CONR?5¿R?6¿; R?3¿ et R?3'¿ représentent séparément H, Ar ou alkyle C¿1-6? éventuellement substitué par OH, NO¿2?, NH¿2?, NR?5¿R?6¿, halogène, CO¿2?R?7¿, CONR?5¿R?6¿ ou Ar, ou alors R?3¿ et R?3'¿ représentent ensemble =O; R?4¿ représente H ou alkyle C¿1-4?, éventuellement substitué par OH, NO¿2?, NH¿2?, NR?5¿R?6¿, halogène, CO¿2?R?7¿, CONR?5¿R?6¿, ou Ar; R?5¿ et R?6¿ représentent séparément H, Ar, alkyle C¿1-6?, HCO, alkyle C¿1-6?-CO, Ar-CO, alkyle C¿1-6?-SO¿2?, ou Ar-SO¿2?; et R?7¿ représente un groupe protecteur à l'acide carboxylique.
Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, 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, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)