Studies On The Synthesis Of HIV-I Reverse Transcriptase Inhibitor Delavirvine Mesylate

Delavirdine is one of the HIV-I Reverse Transcriptase Inhibitors and had been approved by FDA to therapy Acquired Immunodeficiency Syndrome in clinic.A new synthetic route ,based on the reported article ,is designed to prepare Delavirdine mesylate in this paper .As the result ,we get the title compound by optimized 10-step chemical reactions with high yield (17.6%). The structure of title molecule was determined by ¹H-NMR ¹³C-NMR MS and IR.In this paper, Ti (OⁱPr) 4, a potent dehydration,is invented to promote the form of imine thoroughly in the reaction of N- alkylation, Successfully ,we get very pure compound with nearly 100% yield .In addition, the choice of cheap 2-chloro-3-aminopyridine, KBH₄, Raney Ni, catalyzer DMAP , the design of the ration of PPA in 5-nitro indole preparation and study on the condition in other reaction in detail ,all of these endeavor will reduce the price of manufacture in plant practice notably.Recommendablly , we replace the solvent dichloromethane and pyridine used to remove acid form in reaction correspondingly by THF and sodium carbonate in reaction of methanesulfonamination,which lead to obviously decrease the contamination to environment.