Synthesis of [guanido-13C]-γ-hydroxyarginine
- Synthesis of [guanido-13C]-γ-hydroxyarginine
- 윤구; Mark Zabriskie; 천승훈
- carbon-13 synthesis; [guanido-13C]-g-hydroxyarginine; iodolactonization
- Issue Date
- Journal of labelled compounds & radiopharmaceuticals
- VOL 52, NO 2, 53-55
- This report describes an efficient method of synthesizing [guanido-13C]-c-hydroxyarginine HCl salt. Iodolactonization of N-Boc-protected allylglycine mainly provided the cis iodo compound 2. This was converted to an amine through azide 4. The amine 5 was reacted with N-Boc-protected [13C]thiourea to afford N-Boc-protected [13C]guanidine 6, which underwent base catalyzed ring opening. Removal of the N-Boc group afforded [guanido-13C]-c-hydroxyarginine HCl salt 7 giving a 30% overall yield of the final product from N-Boc protected allylglycine 1 in five steps.
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