Verfahren zur Herstellung von Salzen des 4-(2,6-Diamino-pyrimidyl-4-amino)-phenylarsinoxyds

摘要

4 - (2 : 6 - Diamino - 4 - pyrimidylamino)-phenylarsine oxide is prepared by (a) reduction of 4-(2 : 6-diamino-4-pyrimidylamino)-phenyl arsonic acid with sulphur dioxide and hydrochloric acid in the presence of potassium iodide, and hydrolysing the dichloride so formed without purification and isolating the arsine oxide as its carbonate addition salt by passage of CO2 into the alkaline solution; or (b) reacting p-aminophenylarsine oxide with 2 : 6-diamino-4-chloropyrimidine and isolating the required product as its carbonate addition salt. Reaction (b) may be carried out in an acid medium, e.g. aqueous hydrochloric acid. The arsine oxide carbonate addition salt may be converted to the isethionate addition salt by reaction with isethionic acid (see Group VI) in an aqueous medium. Detailed examples are given. U.S.A. Specification 2,435,393 is referred to.ALSO:4 - (2:6 - diamino - 4 - pyrmiidylamino)-phenylarsine oxide and is acid addition salts (see Group IV (b)) may be used in trypanocidal compositions. In particular, the isethionate addition salt may be used in aqueous solution. U.S.A. Specification 2,435,393 is referred to.