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In spite of the impressing cytotoxicity of thapsigargin ( Tg ), this compound cannot be used as a chemotherapeutic drug because of general toxicity, causing unacceptable side effects. Instead, a prodrug targeted towards tumors, mipsagargin, was brought into clinical trials. What substantially reduces the clinical potential is the limited access to Tg and its derivatives and cost-inefficient syntheses with unacceptably low yields. Laser trilobum , which contains a structurally related sesquiterpene lactone, trilobolide ( Tb ), is successfully cultivated. Here, we report scalable isolation of Tb from L. trilobum and a transformation of Tb to 8- O -(12-aminododecanoyl)-8- O -debutanoylthapsigargin in seven steps. The use of cultivated L. trilobum offers an unlimited source of the active principle in mipsagargin.

Large Scale Conversion of Trilobolide into the Payload of Mipsagargin: 8-O-(12-Aminododecanoyl)-8-O-Debutanoylthapsigargin