A microscale synthesis of a promising radiolabelled antitumor drug: Cis‐1,1‐cyclobutanedicarboxylato (2R)‐2‐methyl‐1,4‐butanediamine platinum(II), NK121

Masato Suwa, Osamu Kogawa, Hiroyoshi Nowatari, Yuko Murase, Yoshio Homma, Yutaka Hashimoto

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A promising antitumor drug, cis‐1,1‐cyclobutane‐dicarboxylato (2R)‐2‐methyl‐1,4‐butanediamine platinum(II), NK121, was synthesized from radionuclides of platinum such as 193mPt, 195mPt and 191Pt which were produced by neutron irradiation of enriched 192Pt. The overall yield was 38.6% in a synthesis time of 10 hours. The radioactivities present in 8.39 mg of NK121 were 115.3 μCi as 193mPt, 29.9 μCi as 197Pt, 22.0 μCi as 195mPt, and 4.8 μCi as 191Pt at the end of synthesis. The specific activity of the NK121 was 13.7 μCi (193mPt)/mg NK121 at the end of synthesis. The radiochemical purity of NK121 was typically 99 %. HPLC analyses confirmed that NK121 was in an adequate chemical purity and suitable for animal experimentation.

Original languageEnglish
Pages (from-to)349-354
Number of pages6
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number5
Publication statusPublished - 1992 May



  • NK121
  • Pt‐labelled antitumor drug
  • microscale synthesis

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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