Global Patent Index - EP 1169310 A1

EP 1169310 A1 20020109 - PROCESS FOR PREPARING MKC-442

Title (en)

PROCESS FOR PREPARING MKC-442

Title (de)

VERFAHREN ZU HERSTELLUNG VON MKC-442

Title (fr)

PROCEDE DE PREPARATION DE MKC-442

Publication

EP 1169310 A1 20020109 (EN)

Application

EP 00925979 A 20000413

Priority

  • US 0009965 W 20000413
  • US 12892599 P 19990413

Abstract (en)

[origin: WO0061566A1] A process for preparing 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil, which is also known as MKC-442, is disclosed. The process comprises synthesizing an isopropyl ss-ketoester, such as ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate, using any known method, including from benzyl cyanide and ethyl-2-bromo-3,3-dimethyl-propionate with activated zinc in a Reformatsky reaction. The ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate is then condensed with thiourea in one of two ways. First, the ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate is condensed with thiourea in a two-base system in the presence of a solvent. A second process for condensing the ethyl-2-isopropyl-3-oxo-4-phenyl-butyrate with thiourea is conducted in the presence of potassium t-butoxide to form a benzyl isopropyl thiouracil, which is desulfurized in process step (B). The benzyl isopropyl uracil resulting from either process is then alkoxyalkylated in process to form MKC-442.

IPC 1-7

C07D 239/54

IPC 8 full level

C07D 239/54 (2006.01)

CPC (source: EP KR)

C07D 239/54 (2013.01 - EP KR)

Citation (search report)

See references of WO 0061566A1

Designated contracting state (EPC)

AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

DOCDB simple family (publication)

WO 0061566 A1 20001019; AU 4459000 A 20001114; CA 2369698 A1 20001019; CN 1352637 A 20020605; EP 1169310 A1 20020109; IL 145791 A0 20020725; JP 2002541247 A 20021203; KR 20020040657 A 20020530

DOCDB simple family (application)

US 0009965 W 20000413; AU 4459000 A 20000413; CA 2369698 A 20000413; CN 00806152 A 20000413; EP 00925979 A 20000413; IL 14579100 A 20000413; JP 2000610841 A 20000413; KR 20017012800 A 20011008