Online article for Non-subscribers

Pay per view

Heterocycles has a pay-per-view service for Non-subscribers.
You will be able to directly purchase the full text article through PayPal.
Your purchased Paper can be downloaded after the payment is completed.
An e-mail will be sent the URL to download the paper.
If you have any questions, please contact:

Price: ¥ 4,400 (Yen only)
Period: This Article can be accessed for 7 days.

Short Paper | Regular issue | Vol 92, No. 3, 2016, pp.552-559
Published online, 2nd February, 2016
DOI: 10.3987/COM-15-13397
Synthesis of Novel Benzofuro-Fused Thiazolo[3,2-a]pyrimidinones via Pictet-Spengler Reaction

Dao-Lin Wang,* Dong Wang, Jian-Hua Qiang, and Lin Liu

*Liaoning Key Laboratory of Synthesis and Application of Functional Compound, College of Chemistry & Chemical Engineering, Bohai University, Jinzhou 121001, China


An efficient method for the preparation of novel benzofuro[3’,2’:2,3]pyrido[4,5:d]thiazolo[3,2-a]pyrimidin-5-ones 5 is described. The key intermediate, 7-(3-amino-2-benzofuran)-5H-thiazolo[3,2-a]pyrimidin-5-one (3), was synthesized from 7-(chloromethyl)-5H-thiazolo[3,2-a]pyrimidin-5-one (1) with salicylonitrile (2) by Thorpe-Ziegler isomerization. Subsequent reaction of the intermediate amine with aromatic aldehydes via Pictet-Spengler reaction provided benzofuro-fused thiazolo[3,2-a]pyrimidines under sulfamic acid as catalyst in good yields.