Solid phase synthesis of benzothiazolyl compounds
Solid phase synthesis of benzothiazolyl compounds
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DOI：
10.1016/s0040-4039(01)00109-5
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发表时间：
2001-03-11
影响因子：
1.8
通讯作者：
Barlos, K
中科院分区：
文献类型：
--
作者：
Mourtas, S;Gatos, D;Barlos, K
2-氨基苯硫醇通过其硫醇官能团与2-氯三苯基(CLT)、三叔丁基(TRT)、4-甲氧基三苯基(MMT)和4-甲氧基三苯基(MMT)树脂键合，在氨基上被脂肪酸和芳香酸酰化。用三氟乙酸溶液在二氯甲烷中处理得到的2-N-酰氨基苯硫醇从树脂中解离。从树脂中释放出的2-N-酰基氨基苯硫醇在室温下放置在二硫苏糖醇的DMF或甲醇溶液中1-3h，环化成相应的2-取代苯并噻唑。(C)2001爱思唯尔科学有限公司。保留所有权利。
2-Aminobenzenethiol, bound through its thiol function to the 2-chlorotrityl (Clt)-, trityl (Trt)-, 4-methyltrityl (Mtt)- and 4-methoxytrityl (Mmt)-resins, was acylated at the amino-function by aliphatic and aromatic acids. The obtained 2-N-acylaminobenzenethiols were cleaved from the resin by treatment with trifluoroacetic acid solutions in dichloromethane. The 2-N-acyl-aminobenzenethiols released from the resin were cyclised to the corresponding 2-substituted benzothiazoles, by standing in a solution of dithiothreitol in DMF or methanol for 1-3 h at room temperature. (C) 2001 Elsevier Science Ltd. All rights reserved.