NEW PYRIMIDINE DERIVATIVES
Procedure for the preparation of new pyrimidine derivatives of formula I **(See formula)** in which R1 and R3 signify, independently of each other, each a C1-C4 alkyl radical, which may be unsubstituted or substituted by halogen, cyano, C1-C4alkylthio, cyclopropyl or phenyl; or a C2-C4 alkenyl, C2-C...
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Zusammenfassung: | Procedure for the preparation of new pyrimidine derivatives of formula I **(See formula)** in which R1 and R3 signify, independently of each other, each a C1-C4 alkyl radical, which may be unsubstituted or substituted by halogen, cyano, C1-C4alkylthio, cyclopropyl or phenyl; or a C2-C4 alkenyl, C2-C4 alkynyl or cyclopropyl radical. R2 and R4 independently of one another represent hydrogen or C1-C4 alkyl radicals, X means halogen, an alkoxy radical or a C1-C4 alkylthio radical e Y stands for hydrogen or halogen, which with the condition of/one at least of the substituents R1 and R3 represents the cyclopropyl or cyclopropylalkyl group, and its addition salts with inorganic acids and organic acids, characterized by reacting a 4,6-dichloro-2-amino- pyrimidine or a 4-amino-2,6-dichloro-pyrimidine corresponding to formulas lIa and IIb **(See formula)** where R1 through R4 have the same meaning given in formula I, in an inert organic solvent and in the presence of an acid accepting agent, with a respective amine of formulas IIIa or IIIb **(See formula)** where R1 through R4 have the same meaning given in formula I, and eventually, in the originated 4-chloro-2,6-diamino-pyrimidine, of formula Ia **(See formula)** in which R1 to R4 have the same meaning given above, changing the chlorine atom at position 4, in an inert solvent, for another halogen atom or, in the presence of an acid-accepting agent, for an O1-C4 alkanol radical or C1-C4 alkylthio and/or optionally change the hydrogen atom at position 5, by treatment with halogen or with a halogen donor agent and in an inert organic solvent, with a halogen atom; and, if desired, converting the obtained pyrimidine derivative to an addition salt with an inorganic or organic acid. (Machine-translation by Google Translate, not legally binding) |
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