N-酰基吡唑类化合物的制备及其在合成中的应用

N-酰基吡唑类化合物作为酰化试剂逐步引起了广泛关注,对其制备以及在醇解,氨解,格氏反应,瑞福尔马斯基反应等方面的用途做了探讨.     

Diastereo- and Enantioselective Mannich/Cyclization Cascade Reaction Access to Chiral Benzothiazolopyrimidine Derivatives

An efficient asymmetric Mannich/cyclization cascade strategy was established from 2-benzothiazolimines with N-acylpyrazoles to provide optical active benzothiazolopyrimidine derivatives using a copper-based complex. The mild cascade process constructed various structurally diverse products with broad scope of substrates together with excellent enantioselectivities (up to 99 % ee) and diastereoselectivities (up to 99:1 d.r.).