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一类化学上与半胱氨酸类似的巯基衍生物对于治疗急、慢性支气管炎是有价值的治疗性药物,但是胃肠道的副作用限制了其长期口服治疗。胃肠道不耐受似乎与分子内存在着游离巯基有关,其能粘附于胃肠道的粘蛋白,因此,口服后造成局部损害。由Refarmed与Edmond Pharma公司协作制备了具有保护性巯基的新药。本品是其中最感兴趣的物质。合成由高半胱氨酸硫羟内酯(Ⅰ)起始二步合成得本品(Ⅲ)。Ⅰ在氯仿中用氯乙酰氯酰化至酰胺(Ⅱ)。随后与硫羟乙醇酸作用生成(Ⅲ)。
A class of sulfhydryl derivatives that are chemically cysteine-like is a valuable therapeutic drug for the treatment of acute and chronic bronchitis, but the gastrointestinal side effects limit their long-term oral treatment. Gastrointestinal intolerance appears to be related to the presence of free sulfhydryl groups in the molecule that can adhere to the mucins of the gastrointestinal tract and thus cause local damage after oral administration. New drugs with protective thiols were prepared by Refarmed in collaboration with Edmond Pharma. This product is one of the most interesting substances. Synthesis of homocysteine thiolactone (I) from the initial two-step synthesis of the goods (Ⅲ). I is acylated with chloroacetyl chloride to amide (II) in chloroform. Subsequent interaction with thioglycolic acid (III).