Benzodiazepines are well known class of antianxiety and hypnotic agents. They have replaced the traditional barbiturates and dicarbamates which were used for such treatments in 1990’s. Benzodiazepines are more effective in alleviating anxiety and stress as they have fewer and less severe side effects. BZD’s are also frequently prescribed as drugs for heart and circulatory problems. Objective of this review is to present a literature survey of preparation methods of [1,4] and [1,5]-benzodiazepines and their uses in synthetic organic chemistry. Few of these methods involve minor structural modifications so as to increase polarity, water solubility, metabolic degradation or better metabolic pathway. Some synthetic methods involve combination of pharmacologically active heterocyclic rings such as pyrole, oxadiazole, triazole, tetrazole or imidazole along with diazepine ring which is a promosing drug design strategy for site specificity.
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