Chiral-at-metal strategy was developed to resolve the essential sulfoxide pharmaceutical intermediates R-modafinil acid and its ana-logues with high yields and ee values.The efficient resolution process was achieved b...Chiral-at-metal strategy was developed to resolve the essential sulfoxide pharmaceutical intermediates R-modafinil acid and its ana-logues with high yields and ee values.The efficient resolution process was achieved based on the diastereoselective discrimination caused by hydrogen bond and intramolecular π-π interaction between chiral-at-metal center and the coordinated chiral sulfoxide ligands.Moreover,the chiral Ir(lll)receptor can be reused with complete retention of their configurations and without the loss of reaction activity and enantioselectivity.This work provides a new access to synthesize R-modafinil acid as well as its analogues and develops the application of chiral-at-metal strategy in chiral resolution.展开更多
To the Editor:Generalized pustular psoriasis(GPP)is a rare and severe form of psoriasis for which traditional treatment approaches may not be effective.The traditional approach is systemic treatment with acitretin,met...To the Editor:Generalized pustular psoriasis(GPP)is a rare and severe form of psoriasis for which traditional treatment approaches may not be effective.The traditional approach is systemic treatment with acitretin,methotrexate,and cyclosporin;however,obvious side effects often occur during drug administration,limiting their clinical application.Secukinumab,a fully human anti-interleukin(IL)-17A monoclonal antibody,demonstrates efficacy in treating moderate to severe plaque-type psoriasis.Nonetheless,there are limited evidence-based real-world data on GPP treatment with secukinumab.Two cases of GPP were successfully treated with secukinumab in Peking University Third Hospital recently.This study was approved by the Ethics Committee of our hospital(No.328-01).展开更多
基金the National Natural Science Foundation of China(No.21971266)the Guangdong Provincial Key Platforms and Major Scientific Research Projects of Universities(No.2019KQNCX101)+1 种基金the Pan Deng Project of Guangdong Province(No.pdjh2020b0431)We also thank Dr.Long Jiang from Sun Yat-sen University instrumental analysis and research center.
文摘Chiral-at-metal strategy was developed to resolve the essential sulfoxide pharmaceutical intermediates R-modafinil acid and its ana-logues with high yields and ee values.The efficient resolution process was achieved based on the diastereoselective discrimination caused by hydrogen bond and intramolecular π-π interaction between chiral-at-metal center and the coordinated chiral sulfoxide ligands.Moreover,the chiral Ir(lll)receptor can be reused with complete retention of their configurations and without the loss of reaction activity and enantioselectivity.This work provides a new access to synthesize R-modafinil acid as well as its analogues and develops the application of chiral-at-metal strategy in chiral resolution.
文摘To the Editor:Generalized pustular psoriasis(GPP)is a rare and severe form of psoriasis for which traditional treatment approaches may not be effective.The traditional approach is systemic treatment with acitretin,methotrexate,and cyclosporin;however,obvious side effects often occur during drug administration,limiting their clinical application.Secukinumab,a fully human anti-interleukin(IL)-17A monoclonal antibody,demonstrates efficacy in treating moderate to severe plaque-type psoriasis.Nonetheless,there are limited evidence-based real-world data on GPP treatment with secukinumab.Two cases of GPP were successfully treated with secukinumab in Peking University Third Hospital recently.This study was approved by the Ethics Committee of our hospital(No.328-01).
