1.
Journal of China Pharmaceutical University
;
(6): 297-301, 2009.
Article
in Chinese
| WPRIM
| ID: wpr-480387
ABSTRACT
Aim: To develop a practical synthetic route of raltegravir, a drug for HIV treatment. Methods: Raltegravir was synthesized through an eight-step process including aminonitrile formation, protection with benzyloxy-carbonyl group, conversion of the nitrile to the amidoxime, cyclization to form hydroxypyrimidinone, N-methyla-tion, amidation with microwave-assistance, deprotection, amidation with acyl chloride. Results: The overall yield of the eight-step synthesis is about 12. 0% and the structure of the target compound was confirmed by ~1H NMR, ~(13)C NMR, LR-MS and HR-MS. Conclusion: The reported synthetic process of raltegravir highlights the advantages in terms of readily available starting materials, convenient operation and low cost.