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US 12,466,796 B2Granted
Process for preparing 5-(fluoro-4-imino-3-methyl)-1-tosyl-3,4 dihydropyrimidine-(1H)-one and derivatives of the compound
AssigneeAdama Makhteshim Ltd.
InventorsGal Suez, Samaa Alasibi, Yaakov Mines
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Abstract
The present invention provides a process for preparing a compound having the formula (I): wherein R is alkyl or alkylaryl; each of X1, X2, X3, X4 and X5 is, independently, H, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, alkoxycarbonyl, alkyl carbonyl, hydroxyalkyl, ester, acid halogen, —SH, —OH, —NH2, —NO2, —CN or CF3; Y is O or S; and and Z is a halogen.
Claims14
A process for preparing a compound having the formula (I):
- wherein
- R is alkyl or alkylaryl;
- each of X1, X2, X3, X4 and X5 is, independently, H, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, alkoxycarbonyl, alkyl carbonyl, hydroxyalkyl, ester, a halogen, —SH, —OH, —NH2, —NO2, —CN or CF3;
- Y is O or S;
- and Z is a halogen,
- comprising reacting an alkyl-urea or thiourea of the formula RNH(C═Y) NH2 with a trialkyl orthoformate in the presence of a cyanoacyl derivative having the formula R′C(O)CH2CN, wherein R′ is OH, O—R″ or S—R″, wherein R″ is alkyl, or with a cyanoacetaldehyde dialkyl acetal, under conditions sufficient to obtain the compound of formula (III),
3 more elements
Dependencies are inferred from the claim text.