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Betulin, betulinic acid and their derived compounds are important pentacyclic lupane-type triterpenoids and exhibit diversified pharmacological activities like anti-HIV, antitumor, antimycotic, anti-inflammatory, antioxidant and immunomodulatory activities. Many new methods for the synthesis of potentially valuable betulin derived triterpenoids with potent bioactivity have been largely reported in the past few years. In this review, we will present the progress made on the synthesis of novel structural triterpenoids with excellent chemical or biological activity that have appeared from 2006 to 2012.