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

✍ Scribed by Masato Suwa; Osamu Kogawa; Hiroyoshi Nowatari; Yuko Murase; Yoshio Homma; Yutaka Hashimoto

Publisher
John Wiley and Sons
Year
1992
Tongue
French
Weight
250 KB
Volume
31
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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 ^193m^Pt, ^195m^Pt and ^191^Pt which were produced by neutron irradiation of enriched ^192^Pt. 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 ^193m^Pt, 29.9 μCi as ^197^Pt, 22.0 μCi as ^195m^Pt, and 4.8 μCi as ^191^Pt at the end of synthesis. The specific activity of the NK121 was 13.7 μCi (^193m^Pt)/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.

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