Preparations of Secondary Amines and .beta.-Amino Esters via Additions of Grignard and Reformatsky Reagents to Imines and by One-Pot Reactions of Primary Amines, Aldehydes, and Grignards
摘要:
Additions oi. Grignard and Reformatsky reagents to imines in the presence of 1-(trimethylsilyl)benzotriazole afforded in good yields the corresponding secondary amines and p-amino esters. The procedure is general as imines containing hydrogens a to both carbon and nitrogen can be employed. Extensions of this method to include imines containing other Lewis basic centers, e.g., those derived from furan-, thiophene-, indole-, and p-methoxybenzenecarboxaldehyde, have been successful in avoiding the potential complications which could result from the use of a Lewis acid as the activating : species. The imines need not be isolated, and a one-pot method for the synthesis of secondary amines from aldehydes, primary amines, and Grignard reagents is described.
SUBSTITUTED NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND APPLICATIONS OF ANTITUMOR THEREOF
申请人:Zhejiang University
公开号:EP3124486B1
公开(公告)日:2020-12-09
1-(Trimethylsilyl)benzotriazole-Assisted Addition of Grignard Reagents to Imines: A Versatile Approach to Aliphatic Secondary Amines
作者:Alan R. Katritzky、Qingmei Hong、Zhijun Yang
DOI:10.1021/jo00105a003
日期:1994.12
1-(Trimethylsilyl)benzotriazole-assisted Grignard addition to imines is described.
Phosphatase Binding Compounds and Methods of Using Same
申请人:Yale University
公开号:US20200268897A1
公开(公告)日:2020-08-27
The present invention provides bifunctional compounds that efficiently dephosphorylate certain phospho-activated target proteins. Such target proteins can be any protein involved in the pathway of a disease or disorder, such as but not limited to cancer, neurodegeneration, metabolic disease, diabetes, insulin resistance, and so forth.