Improved synthesis of raltegravir / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 297-301, 2009.
Artículo
en Chino
| 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.
Texto completo:
Disponible
Índice:
WPRIM (Pacífico Occidental)
Idioma:
Chino
Revista:
Journal of China Pharmaceutical University
Año:
2009
Tipo del documento:
Artículo
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