No abstract

methylphosphorothioate is absorbed from the intestine of rats. The distribution pattern shows no accumulation. The main excretory route is through the urine. The metabolic detoxification takes place by the hydrolysis of the methyl phosphate and/or the phenyl phosphate bond. Bromophos or its oxygen analog is not found in the urinary excretion products.O -(4 -Bromo -2,5 -dichlorophenyl) -0,0 -dimethylphosphorothioate, common name Bromophos (30), is a new phosphorothioate insecticide (24) of extremely low mammalian toxicity (12).Bromophos is widely used in public health in controlling mosquitoes and flies (2, 3, 15, 16, 22, 26, 31), in crop protection mainly for the control of vegetable root flies (10,11,14,20), and in storage pest control (13,21) as well as in household insecticides. Since Bromophos is also a very effective agent in the veterinary field (6, 7), its fate in mammals is of interest. MethodsPhosphorus3 2-Labeled Bromophos (Bromophos-P32) was synthesized according to Sehring and Zeile (24),

Die Veresterung von Benzilsäure mit Tropin (Ib) bzw. dem Nortropin‐ Derivat (III) gelingt mit dem Benzilsäureimidazolid (IV).

Five compounds of a group of 2‐(arylimino)‐imidazolidines, among them Clonidine (St 155), have been labeled with 14 in the following manner: Potassium cyanide‐[14C] was converted to potassium thiocyanate‐[14C] and subsequently to the N′‐phenylthiourea using benzoyl chloride and the corresponding aniline. The thiourea was saponified and reacted with methyl iodide to give the quaternary isothiourea derivative. Ring closure to the imidazolidine was achieved through condensation with ethylenediamine. ‐ Tritium labeled Clonidine was obtained by catalytic debromination of the 4‐bromoderivative with tritium gas. ‐ The starting material for deuteroclonidine was ethylene‐[2H4]‐diammonium dichloride.

Hyosine butyl bromide, the active ingredient in Buscopan, is an anticholinergic and antimuscarinic drug used to treat pain and discomfort caused by abdominal cramps. A straightforward synthesis of carbon-14- and deuterium-labeled Buscopan was developed using scopolamine, n-butyl-1- C bromide, and n-butyl- H bromide, respectively. In a second carbon-14 synthesis, the radioactive carbon was incorporated in the tropic acid moiety to follow its metabolism. Herein, we describe the detailed preparations of carbon-14- and deuterium-labeled Buscopan.