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In this work, isolation, purification and biological activity of tagetitoxin has been presented. Then, the previous studies towards the synthesis of the bicyclic core of tagetitoxin have been described. This work describes the retrosynthesis analysis of tagetitoxin to synthesis it in a short and efficient manner. Our synthesis is derived from D-mannose carbohydrate chemistry to access key pyranose intermediate, which could yield advanced intermediates toward the total synthesis of tagetitoxin.