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Machine translation
1. (WO1997021687) PROCESS FOR MAKING DIHYDROPYRIMIDINONES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1997/021687    International Application No.:    PCT/US1996/019651
Publication Date: 19.06.1997 International Filing Date: 12.12.1996
Chapter 2 Demand Filed:    14.07.1997    
IPC:
C07D 239/22 (2006.01)
Applicants: MERCK & CO., INC. [US/US]; 126 East Lincoln Avenue, Rahway, NJ 07065 (US) (For All Designated States Except US).
HU, Essa, H. [US/US]; (US) (For US Only).
SIDLER, Daniel, R. [US/US]; (US) (For US Only).
DOLLING, Ulf, H. [DE/US]; (US) (For US Only).
PATANE, Michael, A. [US/US]; (US) (For US Only)
Inventors: HU, Essa, H.; (US).
SIDLER, Daniel, R.; (US).
DOLLING, Ulf, H.; (US).
PATANE, Michael, A.; (US)
Common
Representative:
MERCK & CO., INC.; 126 East Lincoln Avenue, Rahway, NJ 07065 (US)
Priority Data:
60/008,641 14.12.1995 US
9617968.4 28.08.1996 GB
Title (EN) PROCESS FOR MAKING DIHYDROPYRIMIDINONES
(FR) PROCEDE RELATIF A LA FABRICATION DE DIHYDROPYRIMIDINONES
Abstract: front page image
(EN)The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a $g(b)-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu¿2?O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.
(FR)L'invention concerne un procédé relatif à la fabrication de 5-(alkyle ou alcoxy)carbonyl-6-alkyl-4-(aryle ou alkyle)-3,4-2(1H)-dihydropyrimidinones, en associant un $g(b)-cétoester ou une dione, un aldéhyde et de l'urée en présence d'un réactif au bore, un sel métallique (par exemple, Cu¿2?O) et un catalyseur (par exemple, un acide). Généralement, la réaction est effectuée dans un seul récipient, en présence d'un solvant, ce qui permet d'augmenter le rendement en dihydropyrimidinones et d'obtenir la formation des produits plus facilement qu'avec les méthodes utilisées précédemment.
Designated States: AL, AM, AU, AZ, BA, BB, BG, BR, BY, CA, CN, CU, CZ, EE, GE, HU, IL, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TJ, TM, TR, TT, UA, US, UZ, VN.
African Regional Intellectual Property Organization (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)