Kadry A M, Badawy M A, Hanna H R
Pharmazie. 1986 Aug;41(8):558-9.
2-Methylindole-3-acethydrazide (1) was reacted with arylisothiocyanate to give the corresponding 4-arylthiosemicarbazides 2a-d. Cyclization of the latter gave the corresponding 3-mercapto-5-[3-(2-methylindolyl)methyl]-1,2,4-triazoles 3a-d. Compounds 3a-c reacted with chloroacetic acid to give the corresponding indolyl-1,2,4-triazolythioglycolic acids 4a-c. The methylmercapto derivative 5 was also obtained from 3a and methyliodide. The hydrazide 1 was also reacted with carbon disulfide to give the corresponding indolymethyl-1,3,4-oxadiazole-2-thione (6) which was condensed with piperidine and formaldehyde to give the corresponding Mannich base 7. Condensation of 1 with aromatic aldehydes gave the corresponding hydrazones 8a-c which were converted into the corresponding oxadiazolines 9a-c.
2-甲基吲哚-3-乙酰肼(1)与芳基异硫氰酸酯反应,得到相应的4-芳基硫代氨基脲2a - d。后者环化得到相应的3-巯基-5-[3-(2-甲基吲哚基)甲基]-1,2,4-三唑3a - d。化合物3a - c与氯乙酸反应,得到相应的吲哚基-1,2,4-三唑硫代乙醇酸4a - c。甲基巯基衍生物5也由3a与碘甲烷制得。肼1还与二硫化碳反应,得到相应的吲哚甲基-1,3,4-恶二唑-2-硫酮(6),其与哌啶和甲醛缩合,得到相应的曼尼希碱7。1与芳香醛缩合,得到相应的腙8a - c,其被转化为相应的恶二唑啉9a - c。