Organocatalytic Asymmetric Synthesis Of Benzothiazolopyrimidines Via [4+2] Cyclization Of 2-Benzothiazolimines And Aldehydes
JOURNAL OF ORGANIC CHEMISTRY(2021)
摘要
We report the direct asymmetric synthesis of pyrimido[2,1-b]benzothiazoles using a commercially available chiral amine catalyst. A variety of 2-benzothiazolimines and aldehydes were well tolerated under the reaction conditions and generated the corresponding products in 81-99% yields with excellent diastereoselectivities and enantioselectivities (up to >20:1 dr, 99% ee). Furthermore, the products could be easily converted to other useful chiral building blocks.
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关键词
benzothiazolopyrimidines,cyclization,synthesis
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