（Z）-2-((1H-吲唑-3-基)亚甲基)-6-[¹¹C]甲氧基-7-(哌嗪-1-基甲基)苯并呋喃-3(2H)-酮的合成作为一种新的潜在 PET 探针，用于成像酶 PIM1。
Synthesis of (Z)-2-((1H-indazol-3-yl)methylene)-6-[¹¹C]methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one as a new potential PET probe for imaging of the enzyme PIM1.
机构信息
Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA.
出版信息
Bioorg Med Chem Lett. 2013 Aug 1;23(15):4342-6. doi: 10.1016/j.bmcl.2013.05.091. Epub 2013 Jun 6.
(Z)-2-((1H-Indazol-3-yl)methylene)-6-methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one is a potent and selective proviral integration site in moloney murine leukemia virus kinase 1 (PIM1) inhibitor with an IC₅₀ value of 3 nM. (Z)-2-((1H-Indazol-3-yl)methylene)-6-[(11)C]methoxy-7-(piperazin-1-ylmethyl)benzofuran-3(2H)-one, a new potential PET probe for imaging of the enzyme PIM1, was first designed and synthesized in 20-30% decay corrected radiochemical yield and 370-740 GBq/μmol specific activity at end of bombardment (EOB). The synthetic strategy was to prepare a carbon-11-labeled Boc-protected intermediate followed by a quick acidic de-protection.
（Z）-2-（（1H-吲唑-3-基）亚甲基）-6-甲氧基-7-（哌嗪-1-基甲基）苯并呋喃-3（2H）-酮是一种有效的、选择性的前病毒整合位点莫洛尼鼠白血病病毒激酶 1（PIM1）抑制剂，IC₅₀值为 3 nM。（Z）-2-（（1H-吲唑-3-基）亚甲基）-6-[(11)C]甲氧基-7-（哌嗪-1-基甲基）苯并呋喃-3（2H）-酮，一种新的潜在的用于成像酶 PIM1 的 PET 探针，首先在 20-30%衰变校正放射性化学产率和 370-740GBq/μmol 比活度在末端轰炸（EOB）下设计和合成。合成策略是制备碳-11 标记的 Boc 保护的中间体，然后快速酸性脱保护。
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