Grootveld M C, Razi M T, Sadler P J
Clin Rheumatol. 1984 Mar;3 Suppl 1:5-16. doi: 10.1007/BF03342617.
As used clinically, Myocrisin appears to contain largely polymeric (Autm)n, in which thiomalate (tm) sulphurs bridge between Au(I) ions, together with small amounts of a more reactive gold-bound thiomalate, and free thiomalate, as well as glycerol, unidentified yellow-products from autoclaving and phenylmercury adducts. Solganal usually contains thioglucose sulphinic acid as an impurity. Auranofin, on the other hand, has been crystallised. It is monomeric and Au(I) is almost linearly coordinated by P and S from triethylphosphine and tetraacetyl-beta-D-thioglucose, the latter adopting the chair conformation in the solid state and in solution. The major reaction of auranofin in acidic aqueous solutions appears to be hydrolysis of the sugar acetyl groups but other products arise if methanol is also present in the medium. NMR methods are used to examine in vitro the partition of auranofin between plasma and blood cells. The displacement of the thioglucose ligand and release of PEt3 from gold as OPEt3 are discussed.
在临床应用中，金诺芬似乎主要含有聚合的(Autm)n，其中硫代苹果酸(tm)在金(I)离子之间形成硫桥，还含有少量反应性更强的金结合硫代苹果酸、游离硫代苹果酸、甘油、高压灭菌产生的不明黄色产物以及苯基汞加合物。硫代苹果酸金钠通常含有硫代葡萄糖亚磺酸作为杂质。另一方面，瑞得已结晶。它是单体，金(I)几乎由三乙膦和四乙酰-β-D-硫代葡萄糖中的磷和硫线性配位，后者在固态和溶液中均采用椅式构象。瑞得在酸性水溶液中的主要反应似乎是糖乙酰基的水解，但如果介质中也存在甲醇，则会产生其他产物。核磁共振方法用于体外研究瑞得在血浆和血细胞之间的分配。讨论了硫代葡萄糖配体的置换以及金以OPEt3形式释放出PEt3的情况。
