Indinavir Improved synthesis of Phlong.docVIP

 PAGE \* MERGEFORMAT 10 Indinavir Improved synthesis of Phlong [Abstract] Objective To study the synthesis of indinavir, Phlong method. Methods 2 - acetyl thiophene as raw material, through DMFDMA condensation reaction, hydroxylamine hydrochloride and aminoguanidine nitrate involved cyclization reaction and N-methylation reaction, acetic acid conditions, such as returning a total of seven-step cyclization reaction, synthesis of the target compound Indiplon, as well as the original process has been improved. The results and conclusions of the total yield of the target compound was 40.6%, structure confirmed by MS, NMR spectroscopy and elemental analysis is indeed positive, the line of mild reaction conditions, sources of raw materials convenient, low cost, suitable for industrial production. [Keywords:] medicinal chemistry; preparation; chemical synthesis An improved synthesis method of indilplon [Abstract] Objective To synthesis indiplon.Methods The synthesis started from commercially available of 2-acetylthiophene and dimethylformamide dimethyl acetal by a sequence of reactions including condensation, cyclization, N-methylation.Rusults and Conclusion The overall yield of the synthesis is 40.6%. This approach is industrially applicable for the production of indiplon characterized by its commercially available starting materials, easy purification processes for the synthetic intermediates and highly overall yield of the final product. [Keywords:] medicine chemistry; preparation; chemical synthesis A synthetic route Indinavir, Phlong by the United States Neurocrine Bioscience’s research and development for treatment of insomnia, is expected in October 2006 by the U.S. FDA’s approval. There is no current domestic manufacturers. Indinavir, Phlong a variety of synthetic routes, the author reference [1-6], through analysis and comparison, select the one suitable for industrial production line, and improved them, so that the road has a simple and re