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Industrially viable synthesis of tenofovir a key intermediate of tenofovir disoproxil fumarate and related impurities

Ramadas Chavakula, Narayanarao Mutyala, Srinivasarao Chennupati

An industrially efficient method was developed to synthesize Tenofovir, a key intermediate to tenofovir disoproxil fumarate which is a highly potent antiviral agent. Tenofovir or (R)-9-[2-(phosphonomethoxy) propyl] adenine (2) is synthesized through by condensation of (R)-9-[2- (hydroxyl)propyl]adenine and Diethyl p-toluene sulfonyl oxymethyl phosphonate in presence of 1M dibutyl magnesium (in toluene) in NMPO solvent or mixture of NMPO and tert-butanol and followed by dealkylation with aqHBr. Three known impurities were synthesized and characterized.