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
Life of this patent
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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.
Claims32
1-36. (canceled)
A process for preparing a compound having the formula (I):
- comprising the steps of:
- (ia) reacting an alkyl-urea of the formula RNH(C═Y)NH2 with a trialkyl orthoformate to obtain the compound having the structure:
- (ib) reacting the compound of the formula (VII) with a haloacetonitrile under conditions sufficient to form the compound of the formula (VIII):
- (ii) adding a base to the reaction mixture under conditions sufficient to obtain the compound of formula (III),
- wherein at least one of step (ia), (ib) and (ii) is carried out in the presence of at least one suitable solvent.
39-53. (canceled)
A process for preparing a compound of the formula (II):
- wherein
- R is alkyl or alkylaryl,
- 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.
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A process for preparing a compound of the formula (V):
- wherein
- R is alkyl or alkylaryl;
- and
- Y is O or S,
- 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.
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81-102. (canceled)
Dependencies are inferred from the claim text.