【摘要】 2,3-二疏基丙酸与三氯化锑缩合时形成2-氯-4-羧基-4,5-二氢-1,3-二间硫锑杂茂(Ⅵ:R=H),这个产物的氯原子在水解为羟基时,随同失去一分子水而成为内鹽(Ⅶ)。 2,3-二巯基丁二酸能与酒石酸锑钾起复分解作用,生成环状硫醇盐[4,5-二羧基-4,5-二氢-2-羟基-1,3-二间疏锑杂茂(V)]:但当2,3-二巯基丁二酸与三氯化锑作用,并用碳酸氢钠除去氯化氢时,生成与Friedheim所述“TWSb”(X)成分相同的物质。将内消旋2,5-二巯基已-1,6-二酸与酒石酸锑钾处理时得到4,7-二羧基-1,3-二间硫-2-羟锑杂环庚烷单钾盐(Ⅺ)。这些产物曾用於小白鼠的日本血吸虫病实验治疗,其中Ⅶ及Ⅺ的疗效较酒石酸锑钾为好。更多还原

【Abstract】 Attempts have been made to prepare less toxic antimonials for use in chemotherapy on Schistosomiasis japonicum. It has been established that 2,3-dimercaptopropanol is a powerful antilewisite because it forms a stable ring compound (Ⅱ) with arsenic. It seems reasonable to suppose that analogous cyclic antimony mercaptides (such as Ⅳ and Ⅴ) should be difficult to dissociate and therefore would be less toxic.2,3-Dimercaptopropionic acid was condensed with antimony trichloride, giving 4-carboxyl-2-chloro-4,5-dihydro-1,3-dithiastibiol (Ⅵ; R=H). In an attempt to hydrolyze this compound to form the corresponding 2-hydroxy-derivative (Ⅳ) a mole of water was eliminated, and an inner salt (Ⅶ) resulted.When 2,3-dimercaptosuccinic acid interacted with potassium antimonyltartrate, the corresponding cyclic mercaptide, 4,5-dicarboxyl-4,5-dihydro-2-hydroxy-l,3-dithiastibiol (Ⅴ) was obtained. When, however, the dimercaptosuccinic acid was treated with antimony trichloride in the presence of sodium bicarbonate, a compound corresponding to Friedheim’s "TWSb" (Ⅹ) was formed.Meso-2,5-Dimercaptoadipic acid, on treatment with potassium antimonyltartrate, gave a sevenmembered cyclic mercaptide, 4,7-dicarboxyl-2-hydroxystibino-1,3-dithiacycloheptane (Ⅺ).The activities of these cyclic antimony mercaptides have been tested on mice infected with Schistosomiasis japonicum, and compounds Ⅶ and Ⅺ are more active than tartar emetic, the drug used clinically nowadays in China.更多还原