One-pot SSA-catalyzed b-elimination an efficient and inexpensive through Biotage Initiator耐士科技
2015-02-27 10:38
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资料摘要:
Neu5Ac2en1Me per-OAc, the fully protected glycal of sialic acid, is a key intermediate in the discovery of therapeutics and diagnostics, including anti-influenza drugs and proteolysis resistant peptidomimetic foldamers. The synthesis of this sialic acid derivative, however, still relies on standard sugar chemistry that utilizes multi-step methodologies. Herein we report a facile and highly efficient microwave-assisted preparation of Neu5Ac1Me using silica sulfuric acid (SSA) as solid-supported acid catalyst that is one- to two-orders of magnitude faster than standard procedures. We also describe the microwave-assisted and
SSA-catalyzed one-pot, rapid, solvent free reaction that combines both peracetylation and b-elimination reactions in one step to generate the glycal from Neu5Ac1Me. We coined the term One-pot SSA-catalyzed Technology for b-Elimination Protocol (OneSTEP) to describe this least laborious, most efficient, and practical preparation to date of Neu5Ac2en1Me per-OAc in terms of yield, time, reagent cost, and waste
generation.
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We herein report several highly active catalyst systems with thiadiazolidine 1-oxides as ligands for palladium in the MizorokieHeck reaction. Excellent yields of stilbenes derived from aryl iodides and bromides have been achieved using as little as 0.00002 mol % catalyst. The ligand/palladiumsystem can be stored as a stock solution open to air at room temperature with no observable loss of activity for a period of several months.
耐士科技作为Biotage中国区总代理,以优质的服务为您提供Biotage全系产品以及相关的技术服务。1、开机前确认自动收集机械手臂下无障碍物,试管高度低于机械手臂收集针
2、运行前确认所用流动相充足,废液瓶剩余空间充足
操作步骤:
1.开机,按屏幕左下方黑色电源键
2.进入开机界面后,点击Chemistry进入操作界面
3.在”Method”页面中设定好相关参数
耐士科技作为Biotage中国区总代理,以优质的服务为您提供Biotage全系产品以及相关的技术服务。
操作步骤:
1.开机,按屏幕左下方黑色电源键
2.进入开机界面后,点击
Organic Synthesis
进入编辑界面