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摘要
An efficient method for the preparation of thieno[ 30,20: 2,3] pyrido[ 4,5-d] thiazolo[ 3,2-a] pyrimidin-5ones 5 is described. The key intermediate, 7-(3-amino-4-cyano-5-phenyl aminothieno-2-yl)-5H-thiazolo[ 3,2-a] pyrimidin-5-one (3), wassynthesizedfrom7-chloromethyl-5H-thiazolo[ 3,2-a] pyrimidin-5-one(1) with potassium-(2,2-dicyano-1-phenylaminoethen-1-yl) thiolate (2) by Thorpe-Ziegler isomerization. Subsequent reaction of the intermediate amine with aromatic aldehydes via Pictet-Spengler reaction provided thieno-pyridine fused thiazolo[ 3,2-a] pyrimidines under p-TsOH as catalyst in good yields.
- 出版日期2017-3
- 单位渤海大学
