Terephthaloylamino acids, their salts and esters, and processes for the production thereof
Реферат: The invention comprises tetraiodo-terephthaloyl-amino acids of the general formula <FORM:0836748/IV (b)/1> (wherein R is a hydrogen atom or lower alkyl radical and n is 1 or 2), and lower alkyl esters and metal- and amine-salts of the acids. The invention also comprises the process of producing the above compounds by condensing tetraiodo-terephthaloyl dichloride with an ester or salt of the appropriate amino acid. These tetraiodo-terephthaloyl derivatives are efficient X-ray contrast agents (see Group VI). In Example 1, tetraiodo-terephthaloyl dichloride is dissolved in dimethyl formamide, and the solution is mixed with a solution of glycine in aqueous sodium hydroxide. The mixture is stirred for 2 to 4 hours on a steam-bath. After cooling to 60 DEG C., hydrochloric acid is added, whereupon tetraiodo-terephthalic acid diglycide is precipitated. Example 2 describes the preparation of the corresponding diethyl ester. Example 3 describes the preparation of the bis-diethanolamine salt by dissolving the free acid in somewhat more than the theoretical quantity of 50% aqueous diethanolamine, and precipitating the salt with ethanol. The example also relates to the sodium, lithium and bis-N-methyl-glucamine salts.ALSO:The invention comprises tetraiodo-terephthaloyl-amino acids of the general formula <FORM:0836748/VI/1> (wherein R is a hydrogen atom or lower alkyl radical and n is 1 or 2), and lower alkyl esters and metal- and amine-salts of the acids (see Group IV (b)). The compounds are efficient X-ray contrast agents. In urography, a solution of the sodium, diethanolamine or glucamine salt can be injected intravenously. The compounds may also be used in bronchography and hysterosalpingorraphy. The compounds may be administered orally in the form of solutions, suspensions, tablets or capsules. In bronchography, the esters are preferably used in suspension. It is possible, however, to use salts of the acids provided thickening agents such as methyl cellulose, gelatine or dextran are used.
Process for producing radiohalogenated bioconjugates and products thereof
Номер патента: WO2012022932A1. Автор: Ran Yan,Erik Arstad. Владелец: UCL Business PLC. Дата публикации: 2012-02-23.