Synthesis of 4-Thiazolidineacetic Acids and ß-Homopenicillamine 4-Thiazolidineacetic acids 2, previously unknown homologs of the intensively examined thiazolidine-4-carboxylic acids, were readily prepared by addition of malonic acid to the azomethine group of various 2,5-dihydro-1,3-thiazoles 1, followed by decarboxylation at room temperature. Hydrolysis of 2,2,5,5-tetramethyl-4-thiazolidineacetic acid (2e) lead to ß-homopenicillamine 3, a new homolog of the pharmacologically interesting penicillamine, and its thiolactone hydrochloride 4.
4-Thiazolidineacetic Acids and ß-Homopenicillamine 的合成 4-Thiazolidineacetic Acids 2 是之前未知的
噻唑烷-4-
羧酸的同系物,通过
丙二酸与各种
2,5-二氢-1,3-噻唑 1 的偶
氮甲基相加,然后在室温下进行
脱羧反应,很容易就能制备出来。
2,2,5,5-四
甲基-4-
噻唑烷
乙酸(2e)
水解后可得到 ß-高
青霉胺 3(一种具有药理作用的
青霉胺的新同系物)及其
硫内
酯盐酸盐 4。