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2. Development of new and improved deuteriation and tritiation procedures

Author

Zhong, Desong

Subjects
546.2
Abstract

The thesis is divided into six chapters: Chapter one introduces an overview of deuterium and tritium properties, various labelling procedures as well as analytical methods for hydrogen isotopically labelled compounds. Chapter two describes the preparation of polymer supported transition metal catalysts, particularly rhodium trichloride catalyst, and then applications in the deuteriation and tritiation of aromatic compounds and selected drugs. 3H-NMR spectroscopy showed some aromatic compounds and drugs were labelled with 100% regiospecificity. The regiospecificity was improved when rhodium trichloride was supported on PVP polymer. Chapter three presents a new procedure for the specific incorporation of three tritium atoms into organic compounds. Chapter four describes the applications of a mild Lewis acid catalyst - boron trifluoride etherate in the deuteriation and tritiation of some aromatic compounds and drugs. 2H- and 3H-NMR spectroscopy analysis of the labelled compounds and drugs confirmed the exchange reaction was electrophilic. Chapter five describes a procedure for the synthesis of a deuteriated biocompatible polymer, 2H-PmMl2. When the procedure was adopted for the synthesis of the tritiated version, the polymer was labelled with very low specific activity. A microwave assisted procedure was investigated to see whether the deuteriation of the monomer, HEMA-PC could be achieved by this method. In chapter six NMR spectroscopy is employed to study methylation kinetics using methyl triflate as methylating reagent.

Published
1997

6. Synthesis of [3 H] and [14 C]genipin

Author

Queen, Adele.E., primary, Hesk, David, additional, Lindsay, David.M., additional, Kerr, William.J., additional, Rehder, Kenneth, additional, Fennell, Tim, additional, Mascarella, Wayne, additional, Zhong, Desong, additional, and Runyon, Scott, additional

Published
2020
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7. Contributors

Author

Ando, Isao, primary, Aoki, Akira, additional, Asakura, Tetsuo, additional, Asano, Tsushi, additional, Bloxsidge, J.P., additional, Blümich, Bernhard, additional, Blümer, P., additional, Cross, Timothy A., additional, Demura, Makoto, additional, Ernst, Matthias, additional, Gerstein, Bernard C., additional, Grage, S.L., additional, Harris, Robin K., additional, Holstein, Peter, additional, Horii, Fumitaka, additional, Inoue, Yoshio, additional, Ito, Takuro, additional, Jones, John R., additional, Kameda, Tsunenori, additional, Kuroki, Shigeki, additional, kurosu, hiromichi, additional, Law, Robert V., additional, Masuda, Kenji, additional, Maciel, Gary E., additional, Matsukawa, Shingo, additional, Meier, Beat H., additional, Monti, Gustavo A., additional, Naito, Akira, additional, Nishikawa, Naoki, additional, Russell, Jeremy C., additional, Saito, Hajime, additional, Sharratt, A.P., additional, Sherrington, David C., additional, Takayama, Toshio, additional, Takegoshi, Kiyonori, additional, Tuzi, Satoru, additional, Ulrich, Anne S., additional, Vick, T.A., additional, Yamanobe, Takeshi, additional, Yasunaga, Hidekazu, additional, Yoshimizu, Hiroaki, additional, Webb, Graham A., additional, Whittaker, Andrew K., additional, and Zhong, Desong, additional

Published
1998
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8. Synthesis of [3H] and [14C]genipin.

Author

Queen, Adele.E., Hesk, David, Lindsay, David.M., Kerr, William.J., Rehder, Kenneth, Fennell, Tim, Mascarella, Wayne, Zhong, Desong, and Runyon, Scott

Subjects
HYDROGEN isotopes, DEUTERIUM, TRITIUM, ISOTOPE exchange reactions, METHYL formate, CYANIDES
Abstract

[3H]Genipin was synthesized in a single step by Ir(I) catalyzed hydrogen isotope exchange. Conditions for selective exchange of the sp2 CH bond ortho to the methyl ester functionality were developed through deuterium modeling studies through a catalyst screen. Optimized conditions so obtained were then utilized with tritium gas to generate [3H]genipin at a specific activity of 18.5 Ci/mmol. Racemic [14C]genipin was prepared in eight steps in overall 5.4% radiochemical yield from potassium [14C]cyanide. [ABSTRACT FROM AUTHOR]

Published
2020
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10. Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-[(1S,3aS)-2,3,3a,4,5,6-Hexahydro-1H-phenalen-1-yl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (Ro 64-6198)

Author

Chang, Steven D., primary, Brieaddy, Lawrence E., additional, Harvey, Joseph D., additional, Lewin, Anita H., additional, Mascarella, S. Wayne, additional, Seltzman, Herbert H., additional, Reddy, P. Anantha, additional, Decker, Ann M., additional, McElhinny, Charles J., additional, Zhong, Desong, additional, Peterson, Elisha E., additional, Navarro, Hernán A., additional, Bruchas, Michael R., additional, and Carroll, F. Ivy, additional

Published
2015
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11. Development of new and improved deuteriation and tritiation procedures

Author

Zhong, Desong.

Abstract

The thesis is divided into six chapters: Chapter one introduces an overview of deuterium and tritium properties, various labelling procedures as well as analytical methods for hydrogen isotopically labelled compounds. Chapter two describes the preparation of polymer supported transition metal catalysts, particularly rhodium trichloride catalyst, and then applications in the deuteriation and tritiation of aromatic compounds and selected drugs. 3H-NMR spectroscopy showed some aromatic compounds and drugs were labelled with 100% regiospecificity. The regiospecificity was improved when rhodium trichloride was supported on PVP polymer. Chapter three presents a new procedure for the specific incorporation of three tritium atoms into organic compounds. Chapter four describes the applications of a mild Lewis acid catalyst - boron trifluoride etherate in the deuteriation and tritiation of some aromatic compounds and drugs. 2H- and 3H-NMR spectroscopy analysis of the labelled compounds and drugs confirmed the exchange reaction was electrophilic. Chapter five describes a procedure for the synthesis of a deuteriated biocompatible polymer, 2H-PmMl2. When the procedure was adopted for the synthesis of the tritiated version, the polymer was labelled with very low specific activity. A microwave assisted procedure was investigated to see whether the deuteriation of the monomer, HEMA-PC could be achieved by this method. In chapter six NMR spectroscopy is employed to study methylation kinetics using methyl triflate as methylating reagent.

Published
1997

13. A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay

Author

Smith, Emilie D., primary, Ariane Vinson, N., additional, Zhong, Desong, additional, Berrang, Bertold D., additional, Catanzaro, Jennifer L., additional, Thomas, James B., additional, Navarro, Hernán A., additional, Gilmour, Brian P., additional, Deschamps, Jeffrey, additional, and Carroll, F. Ivy, additional

Published
2008
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17. Synthesis of 3β-(4-[<SUP>125</SUP>I]iodophenyl)tropane-2-β-pyrrolidine carboxamide ([<SUP>125</SUP>I]RTI-229)

Author

Zhong, Desong, Kotian, Pravin, Wyrick, Christopher D., Seltzman, Herbert H., Kepler, John A., Kuhar, Michael J., Boja, John W., and Carroll, F. Ivy

Abstract

A WIN 35,065-2 analog, 3β-(4-iodophenyl)tropane-2β-pyrrolidine carboxamide (RTI-229), has been radiolabelled with iodine-125 by radioiododestannylation of the corresponding trimethyltin derivative using carrier-free sodium iodide-125 as the isotope source. Purification by reversed-phase HPLC gives [125I]RTI-229 in good yield (89·4%) with high radiochemical purity (>99%) and high specific activity (2125 mCi/μmol, 78·6 GBq/μmol, based on the specific activity of the Na125I used). Copyright © 1999 John Wiley & Sons, Ltd.

Published
1999
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18. High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): A high-affinity 5-HT2A receptor-selective agonist radioligand

Author

Nichols, David E., Frescas, Stewart P., Chemel, Benjamin R., Rehder, Kenneth S., Zhong, Desong, and Lewin, Anita H.

Subjects
*CELL lines, *ANTIHYPERTENSIVE agents, *SEROTONIN antagonists, *CELL culture
Abstract

Abstract: The title compound ([3H]INBMeO) was prepared by an O,O-dimethylation reaction of a t-BOC protected diphenolic precursor using no carrier added tritiated iodomethane in DMF with K2CO3. Removal of the t-BOC protecting group and purification by HPLC afforded an overall yield of 43%, with a radiochemical purity of 99% and specific activity of 164Ci/mmol. The new radioligand was suitable for labeling human 5-HT2A receptors in two heterologous cell lines and had about 20-fold higher affinity than [3H]ketanserin. [Copyright &y& Elsevier]

Published
2008
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19. Caged Naloxone: Synthesis, Characterization, and Stability of 3- O-(4,5-Dimethoxy-2-nitrophenyl)carboxymethyl Naloxone (CNV-NLX).

Author

Lewin AH, Fix SE, Zhong D, Mayer LD, Burgess JP, Mascarella SW, Reddy PA, Seltzman HH, and Carroll FI

Subjects
Analgesics, Opioid chemistry, Methanol chemistry, Ultraviolet Rays, Light, Naloxone analogs & derivatives, Naloxone chemistry, Narcotic Antagonists chemistry
Abstract

The photolabile analogue of the broad-spectrum opioid antagonist naloxone, 3- O-(4,5-dimethoxy-2-nitrophenyl)carboxymethyl naloxone (also referred to as "caged naloxone", 3- O-(α-carboxy-6-nitroveratryl)naloxone, CNV-NLX), has been found to be a valuable biochemical probe. While the synthesis of CNV-NLX is simple, its characterization is complicated by the fact that it is produced as a mixture of α R,5 R,9 R,13 S,14 S and α S,5 R,9 R,13 S,14 S diastereomers. Using long-range and heteronuclear NMR correlations, the 1 H NMR and 13 C NMR resonances of both diastereomers have been fully assigned, confirming the structures. Monitoring of solutions of CNV-NLX in saline buffer, in methanol, and in DMSO has shown CNV-NLX to be stable for over a week under fluorescent laboratory lights at room temperature. Exposure of such solutions to λ 365 nm from a hand-held UV lamp led to the formation of naloxone and CNV-related breakdown products.

Published
2018
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