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1. (WO2006017045) FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2006/017045    International Application No.:    PCT/US2005/023514
Publication Date: 16.02.2006 International Filing Date: 01.07.2005
IPC:
C07C 233/00 (2006.01), C07D 211/72 (2006.01)
Applicants: MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US) (For All Designated States Except US).
CAMPOS, Kevin, R. [US/US]; (US) (For US Only).
KLAPARS, Artis [LV/US]; (US) (For US Only).
MCWILLIAMS, J. Christopher [US/US]; (US) (For US Only).
SHULTZ, C. Scott [US/US]; (US) (For US Only).
WALLACE, Debra, J. [GB/GB]; (GB) (For US Only).
CHEN, Alex, M. [CN/US]; (US) (For US Only).
FREY, Lisa, F. [US/US]; (US) (For US Only).
PERESYPKIN, Andrey, V. [RU/US]; (US) (For US Only).
WANG, Yaling [CN/US]; (US) (For US Only).
WENSLOW, Robert, M. [US/US]; (US) (For US Only).
CHEN, Cheng-Yi [US/US]; (US) (For US Only)
Inventors: CAMPOS, Kevin, R.; (US).
KLAPARS, Artis; (US).
MCWILLIAMS, J. Christopher; (US).
SHULTZ, C. Scott; (US).
WALLACE, Debra, J.; (GB).
CHEN, Alex, M.; (US).
FREY, Lisa, F.; (US).
PERESYPKIN, Andrey, V.; (US).
WANG, Yaling; (US).
WENSLOW, Robert, M.; (US).
CHEN, Cheng-Yi; (US)
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US)
Priority Data:
60/586,306 08.07.2004 US
Title (EN) FORMATION OF TETRA-SUBSTITUTED ENAMIDES AND STEREOSELECTIVE REDUCTION THEREOF
(FR) FORMATION D'ENAMIDES TETRA-SUBSTITUES ET REDUCTION STEREOSELECTIVE DE CES DERNIERS
Abstract: front page image
(EN)The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
(FR)La présente invention concerne un procédé pratique de préparation d'un énamide (II) par couplage catalysé par le palladium d'un amide primaire (IV) avec un composé de formule structurale (III). L'invention concerne également des formes cristallines d'un composé produit selon ledit procédé, en particulier, une forme cristalline anhydre, forme B, ainsi que des solvates cristallins correspondant à trois modèles, type 1, type 2 et type 3 et des composés intermédiaires cristallins produits lors de la mise en oeuvre du procédé. La présente invention concerne enfin la réduction stéréosélective de l'énamide tétrasubstitué (II) en amide correspondant (I).
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, 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)