A Simple and New Method for the Synthesis of 1,5-Benzodiazepine and its Derivatives

Author(s): Pratima Sharma, Navneet Kumar, Rachna Mishra, Aastha Pareek and Dharm Kishore

Delavirdine has been recently approved by FDA for its application in the treatment of AIDS. As its efficacy has been lower than ot her approved NNRTIs, therefore, its use was not recommended as a part of initial therapy but in combination of other drugs. To circumvent this therapeutic difficulty, a search of new delavirdine analogue with enhanced activity was pursued. A survey on the other recently FDA approved NNRTs revealed that a pyrimidine derivative ‘etravirine’ has emerged as one of the most potent and powerful anti-HIV agent. This discovery provided optimism that a better analogue of delavirdine could perhaps be developed by substituting pyrimidine nucleus in its molecule. We report in this communication, the preliminary results of the study focused in the direction of designing an amended analogue of delavirdine, in which the pyridine part of the delavirdine was replaced by pyrimidine nucleus.

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