An efficient and practical radiosynthesis of [11C]temozolomide

Org Lett. 2012 Dec 7;14(23):5872-5. doi: 10.1021/ol302791x. Epub 2012 Nov 14.

Abstract

Temozolomide (TMZ) is a prodrug for an alkylating agent used for the treatment of malignant brain tumors. A positron emitting version, [(11)C]TMZ, has been utilized to help elucidate the mechanism and biodistribution of TMZ. Challenges in [(11)C]TMZ synthesis and reformulation make it difficult for routine production. A highly reproducible one-pot radiosynthesis of [(11)C]TMZ with a radiochemical yield of 17 ± 5% and ≥97% radiochemical purity is reported.

MeSH terms

  • Antineoplastic Agents, Alkylating / chemical synthesis*
  • Antineoplastic Agents, Alkylating / chemistry
  • Antineoplastic Agents, Alkylating / pharmacology
  • Brain Neoplasms / drug therapy*
  • Carbon Radioisotopes / chemistry
  • Dacarbazine / analogs & derivatives*
  • Dacarbazine / chemical synthesis
  • Dacarbazine / chemistry
  • Dacarbazine / pharmacology
  • Molecular Structure
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Radiopharmaceuticals / pharmacology
  • Temozolomide
  • Tissue Distribution

Substances

  • Antineoplastic Agents, Alkylating
  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Dacarbazine
  • Temozolomide