Structural Studies on Bioactive Compounds. Part 37.1 Suzuki Coupling of Diaminopyrimidines: A New Synthesis of the Antimalarial Drug Pyrimethamine
- 1 October 2002
- journal article
- research article
- Published by SAGE Publications in Journal of Chemical Research
- Vol. 2002 (10), 482-484
- https://doi.org/10.3184/030823402103170664
Abstract
Suzuki reactions have been used successfully to effect cross-coupling of 5-halopyrimidines with 4-chlorobenzeneboronic acid and 2,4-diamino-5-(4-chloro-3-halo)-6-ethylpyrimidines with 4-methoxybenzeneboronic acid. The antimalarial drug pyrimethamine has been prepared by coupling 2,4-diamino-6-ethyl-5-iodopyrimidine with 4-chlorobenzeneboronic acid.Keywords
This publication has 6 references indexed in Scilit:
- Structural Studies on Bioactive Compounds. Part 36: Design, Synthesis and Biological Evaluation of Pyrimethamine-Based Antifolates Against Pneumocystis cariniiBioorganic & Medicinal Chemistry, 2002
- Structural studies on bioactive compounds. Part 29Bioorganic & Medicinal Chemistry, 2000
- Synthesis of 5-Aryluridines and 5-Aryl-2′-deoxyuridinesSynthetic Communications, 1990
- Structural studies on bioactive compounds. 8. Synthesis, crystal structure and biological properties of a new series of 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against a methotrexate-resistant tumor cell lineJournal of Medicinal Chemistry, 1989
- A New and Facile Synthesis of 5-Arylpyrimidines and 4-ArylpyrazolesHETEROCYCLES, 1982
- 2,4-Diaminopyrimidines as Antimalarials. III. 5-Aryl DerivativesJournal of the American Chemical Society, 1951