Back to results
US 4,902,796 AGranted
6-alkenyl and ethynyl derivatives of 2-amino-4-hydroxypyrido[2,3-d]pyrimidines
AssigneeThe Trustees of Princeton University
InventorsEdward C. Taylor, George S. K. Wong
Life of this patent
Estimating the term…
Abstract
2-Amino-4-hydroxy-6-[2-(4-carboxyphenyl)alk-1-en-1-yl]pyrido[2,3,-d]pyrimid ines and 2-amino-4-hydroxy-6-[2-(4-carboxyphenyl)alk-1-yn-1-yl]pyrido[2,3-d]pyrimid ines are prepared through the reaction of a halo-aromatic compound and an unsaturated compound in the prosence of a palladium catalyst. The products are chemical intermediates for the preparation of antineo-plastic agents. A typical embodiment is the reaction of a protected 2-amino-4-hydroxy-6-ethynylpyrido[2,3-d]pyrimidine and an ester of 4-iodobenzoic acid.
Claims18
A compound of the formula:
- ##STR14## wherein R.sup.1 is --NHCH(COOR.sup.2)CH.sub.2 CH.sub.2 COOR.sup.2, or OR.sup.2 in which R.sup.2 is hydrogen or a carboxylic acid protecting group;
- and
- R.sup.4 is hydrogen or an amino protecting group.
A compound of the formula:
- ##STR15## wherein R.sup.4 is hydrogen or an amino protecting group;
- Z.sup.1 when taken independently of Z.sup.2 is hydrogen;
- and
- Z.sup.2 when taken independently of Z.sup.1 is hydrogen, methyl or ethyl;
- or
- Z.sup.1 and Z.sup.2 when taken together are a carbon-carbon bond.
3 more elements
Dependencies are inferred from the claim text.