Tritiated guanethidine of high specific activity
β Scribed by Steven D. Wyrick; A. Wayne Pittman; Larry J. Loeffler
- Publisher
- John Wiley and Sons
- Year
- 1983
- Tongue
- French
- Weight
- 310 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0022-2135
No coin nor oath required. For personal study only.
β¦ Synopsis
Due to the desire for biological assay techniques of greater sensitivity and specificity than presently exist for the antihypertensive drug guanethidine, tritium labeled guanethidine of high specific activity was prepared for use in radioimmunoassay procedures. This drug has been labeled in other positions than described here resulting in much lower specific activity and less than optimal sensitivity in RIA work. The work described here involves the preparation, deuteration and tritiation of an olef inic precursor, N-(2-aminoethy1)-A4hexahydroazocine which was converted in one subsequent step to tritiated guanethidine with a specific activity of 72 Ci/mmole (145 mCi/mg) for the sulfate salt and 36 Ci/mmole (182 mCi/mg) for the free base.
π SIMILAR VOLUMES
## Abstract Tritiated methoxamine with a specific activity of 28.5 Ci/mmol was prepared by iodination of methoxamine followed by catalytic tritiation.
## Abstract The synthesis of the trichloromethyl analogue of benzyloxycarbonylβthreonine is described. This precursor was reduced by tritium gas to give [methylβ^3^H~3~]βthreonine and its allo isomer. They were separated by HPLC using a chiral stationnary phase. They have a molar specific activity
Thiomethylenes-3 H] CEP-1347 (5) was synthesized by the tritiation of diformyl precursor 3 with NaB 3 H 4 followed by treatment with ethanethiol. [Methyl ester-3 H] CEP-1347 ( 7) was prepared at even higher specific activity by the alkylation of precursor 6 with C 3 H 3 I.