Process for the preparation of pyrimidine derivatives
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United States of America Patent
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Dec 25, 2007
Grant Date -
Jun 9, 2005
app pub date -
Dec 3, 2004
filing date -
Dec 4, 2003
priority date (Note) -
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Abstract
An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula ##STR00001## wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R.sup.1 is a substituted or unsubstituted hydrocarbon group, R.sup.2 and R.sup.3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula ##STR00002## wherein R.sup.4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R.sup.5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R.sup.5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R.sup.5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolyzable protecting group; in the presence of a base.
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