Process for the preparation of fused pyridine compounds

Details Process for the preparation of fused pyridine compounds Process for the preparation of fused pyridine compounds

1988-08-08

1991-01-29

Shah, Mukund J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544257, 546350, C07D47104

Patent

active

049888137

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 through the reaction of a haloaromatic compound and an unsaturated compound in the presence of a palladium catalyst. The products are chemical intermediates for the preparation of antineoplastic 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.

REFERENCES:
Sakamoto et al., "A Facile Synthesis of Ethynyl-Substituted Six-Membered N-Heteroaromatic Compounds", Synthesis, 1983. p. 312.
Edo et al., Chem. Abstr. 91: 20435c.

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