Simple and efficient method for the synthesis of 2′, 3′-didehydro-3′-deoxythymidine (d4T)

R Paramashivappa, PP Kumar, PVS Rao, AS Rao

Index: Paramashivappa; Phani Kumar; Subba Rao; Srinivasa Rao Tetrahedron Letters, 2003 , vol. 44, # 5 p. 1003 - 1005

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Citation Number: 13

Abstract

2′, 3′-Didehydro-3′-deoxythymidine (d4T) is an orally active antiviral drug used in the treatment of AIDS. A novel two-step synthetic method was developed for the synthesis of d4T using inexpensive reagents. An improvement in the yield was achieved for the conversion of the intermediate oxetane to d4T. This is the first simple and efficient method for the large- scale synthesis of d4T.