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Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor
Organic Letters ( IF 5.2 ) Pub Date : 2018-05-22 00:00:00 , DOI: 10.1021/acs.orglett.8b01316
Xiaoze Bao 1 , Shiqiang Wei 1 , Xingkai Qian 2 , Jingping Qu 1 , Baomin Wang 1 , Liwei Zou 2 , Guangbo Ge 2
Affiliation  

A catalytic asymmetric [3 + 2] cyclization of novel 4-isothiocyanato pyrazolones and isatin-derived ketimines was developed, delivering a wide range of intriguing dispirotriheterocyclic products in high yield with excellent diastereoselectivity and enantioselectivity. A chiral sulfoxide derivative of this dispirocyclic product was identified to be a promising hit of the human carboxylesterase 1 inhibitor, and the significant difference of the activity between two enantiomers emphasized the importance of this asymmetric process.

中文翻译:

含多药基双螺三杂环支架的不对称构建和人类羧基酯酶1抑制剂的鉴定。

开发了新型4-异硫氰酸根并吡唑酮和伊斯汀衍生的酮亚胺的催化不对称[3 + 2]环化反应,以高收率提供了多种引人入胜的双螺三杂环产品,具有出色的非对映选择性和对映选择性。该双螺环产物的手性亚砜衍生物被认为是人羧化酶1抑制剂的有前途的产物,并且两种对映异构体之间活性的显着差异强调了这种不对称过程的重要性。
更新日期:2018-05-22
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