PRACTICAL SYNTHESIS OF THE ANTI-HIV DRUG, PMPA

The anti-HIV nucleotide analogue PMPA can be prepared on a kilogram-sc ale by a three step sequence: i) condensation of adenine with (R)-prop ylene carbonate, ii) alkylation of the resulting (R)-9-(2-hydroxypropy l)adenine with diethyl p-toluenesulfonyloxymethanephosphonate using li thium tert-butoxide and iii) cleavage of the phosphonate ester functio nalities with bromotrimethylsilane. (C) 1998 Elsevier Science Ltd. All rights reserved.