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Radioiodination of 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine, 4-(3-iodobenzyl)-1-(benzylsulfonyl)piperazine and their derivatives via isotopic and non-isotopic exchange reactions
- 作者：Masoud Sadeghzadeh (1)
Fariba Johari Daha (1)
Shahab Sheibani (1)
Mostafa Erfani (1)
- 关键词：Radioiodination ; Isotopic and non ; isotopic exchange ; 125I ; 4 ; Benzyl ; 1 ; (3 ; iodobenzylsulfonyl)piperidine ; 4 ; (3 ; Iodobenzyl) ; 1 ; (benzylsulfonyl)piperazine ; Sigma ; 1 receptor ligands
- 刊名：Journal of Radioanalytical and Nuclear Chemistry
- 出版年：2014
- 出版时间：December 2014
- 年：2014
- 卷：302
- 期：3
- 页码：1119-1125
- 全文大小：252 KB
- 参考文献：1. Koehler L, Gagnon K, McQuarrie S, Wuest F (2010) Molecules 15:2686-718 CrossRef
2. Eersels JLH, Travis MJ, Herscheid JDM (2005) J Label Compd Radiopharm 48:241-57 CrossRef
3. Seevers RH, Counsell RE (1982) Chem Rev 82:575-90 CrossRef
4. R?nnest MH, Nissen F, Pedersen PJ, Larsen TO, Mier W, Clausen MH (2013) Eur J Org Chem 2013:3970-973 CrossRef
5. Eisenhut M, Hull WE, Mohammed A, Mier W, Lay D, Just W, Gorgas K, Lehmann WD, Haberkorn U (2000) J Med Chem 43:3913-922 CrossRef
6. Vaidyanathan G, White B, Affleck DJ, McDougald D, Zalutsky MR (2011) Nucl Med Biol 38:77-2 CrossRef
7. Akgu E, Portoghese PS, Sajjad M, Nabi HA (2007) J Label Compd Radiopharm 50:165-70 CrossRef
8. Kabalka GW, Yao ML, Akula MR, Yong L (2012) Pure Appl Chem 84:2309-315 CrossRef
9. Akula MR, Yao ML, Kabalka GW (2011) J Label Compd Radiopharm 54:132-34 CrossRef
10. Stahlschmidt A, Machulla H-J, Reischl G, Knaus EE, Wiebe LI (2008) Appl Radiat Isot 66:1221-228 CrossRef
11. Tsopelas C (1999) Nucl Med Biol 26:591-95 CrossRef
12. Schneider RF, Engelhardt EL, Stobbe CC, Fenning MC, Chapman JD (1997) J Label Compd Radiopharm 39:541-57 CrossRef
13. Wafelman AR, Konings MCP, Hoefnagel CA, Maes RAA, Beijnen JH (1994) Appl Radiat Isot 45:997-007 CrossRef
14. Liefhold J, Eisenhut M (1986) J Label Compd Radiopharm 23:1239
15. Eisenhut M (1982) Int J Appl Radiat Isot 33:499-04 CrossRef
16. Adam MJ, Wilbur DS (2005) Chem Soc Rev 34:153-63 CrossRef
17. Farah K, El-Mohty AA, El-Ghany EA (1999) J Radioanal Nucl Chem 240:243-49 CrossRef
18. Owens J, Murray T, McCulloch J, Wyper D (1992) J Label Compd Radiopharm 31:45-0 CrossRef
19. Martin WR, Eades CG, Thompson JA, Huppler RE, Gilbert PE (1976) J Pharmac Exp Ther 197:517-32
20. Abou-Gharbia M, Ablordeppey SY, Glennon RA (1993) Annu Rep Med Chem 28:1-0 CrossRef
21. Guitart X, Codony X, Monroy X (2004) Psychopharmacology 174:301-19 CrossRef
22. Hou C, Tu Z, Mach R, Kung HF, Kung M-P (2006) Nucl Med Biol 33:203-09 CrossRef
23. Akhter N, Shiba K, Ogawa K, Tsuji S, Kinuya S, Nakajima K, Mori H (2008) Nucl Med Biol 35:29-4 CrossRef
24. Kawamura K, Kubota K, Kobayashi T, Elsinga PH, Ono M, Maeda M, Ishiwata K (2005) Ann Nucl Med 19:701-09
文摘
A mild and simple technique for preparing of 4-benzyl-1-(3-[125I]iodobenzylsulfonyl)piperidine, 4-(3-[125I]iodobenzyl)-1-(benzylsulfonyl)piperazine and their derivatives, as sigma-1 receptor ligands, with relatively high radiochemical yields via nucleophilic substitution reaction by means of isotopic and non-isotopic exchange reactions is described. Some factors affecting the radiochemical yield were commonly studied in presence of acidic medium at elevated temperature. Unfortunately, the radiochemical yields were weak. Some attempts were carried out in presence of polar aprotic solvents to enhance the radiochemical yield. N,N-Dimethylformamide was proved highly efficient for preparing of radioiodinated 4-benzyl-1-(3-iodobenzylsulfonyl)piperidine (4-B-[125I]-IBSP, 70?±?5.7?%) and 4-(3-iodobenzyl)-1-(benzylsulfonyl)piperazine (4-[125I]-IBBSPz, 72?±?6.0?%) at moderate temperature (100-05?°C) within 8?h. The specific activities of 4-B-[125I]-IBSP and 4-[125I]-IBBSPz (6,534.2 and 5,927.4?MBq/mmol) were obtained respectively.
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