EP 0882026 A4 19990407 - PROCESS FOR MAKING DIHYDROPYRIMIDINONES
Title (en)
PROCESS FOR MAKING DIHYDROPYRIMIDINONES
Title (de)
VERFAHREN ZUR HERSTELLUNG VON DIHYDROPYRIMIDONEN
Title (fr)
PROCEDE RELATIF A LA FABRICATION DE DIHYDROPYRIMIDINONES
Publication
Application
Priority
- GB 9617968 A 19960828
- US 9619651 W 19961212
- US 864195 P 19951214
Abstract (en)
[origin: WO9721687A1] 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 beta -keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu2O) 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.
IPC 1-7
IPC 8 full level
C07D 239/36 (2006.01); C07B 61/00 (2006.01); C07D 239/22 (2006.01)
CPC (source: EP KR)
C07D 239/22 (2013.01 - EP KR)
Citation (search report)
- [A] EP 0157219 A1 19851009 - SUNTORY LTD [JP]
- [DA] US 4675321 A 19870623 - BALDWIN JOHN J [US], et al
- [A] C.O. KAPPE: "100 YEARS OF THE BIGINELLI DIHYDROPYRIMIDINE SYNTHESIS", TETRAHEDRON, vol. 32, 1993, pages 6937 - 63, XP002092173
- [DA] H. CHO ET AL.: "Dihydropyrimidines: novel Calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity", JOURNAL OF MEDICINAL CHEMISTRY, vol. 32, no. 10, 1989, pages 2399 - 2406, XP002092174
- See references of WO 9721687A1
Designated contracting state (EPC)
AT BE CH DE DK ES FI FR GB GR IE IT LI LU NL PT SE
DOCDB simple family (publication)
WO 9721687 A1 19970619; AU 1331697 A 19970703; AU 705409 B2 19990520; BR 9611933 A 19990302; CA 2238924 A1 19970619; CZ 184098 A3 19981111; EP 0882026 A1 19981209; EP 0882026 A4 19990407; JP 2000501734 A 20000215; KR 19990072125 A 19990927; MX 9804766 A 19981031; NZ 326039 A 19990830; PL 327147 A1 19981123; SK 77398 A3 19990211
DOCDB simple family (application)
US 9619651 W 19961212; AU 1331697 A 19961212; BR 9611933 A 19961212; CA 2238924 A 19961212; CZ 184098 A 19961212; EP 96944785 A 19961212; JP 52216197 A 19961212; KR 19980704443 A 19980613; MX 9804766 A 19980612; NZ 32603996 A 19961212; PL 32714796 A 19961212; SK 77398 A 19961212