6436-90-4Relevant articles and documents
EIF4E INHIBITORS AND USES THEREOF
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Paragraph 00337; 00363; 00373, (2021/09/11)
The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
N-benzyl glycine ethyl ester preparation and purification method
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Paragraph 0034-0039; 0041-0043, (2020/02/14)
The invention provides an N-benzyl glycine ethyl ester preparation and purification method, which comprises: preparing a N-benzyl glycine ethyl ester hydrochloride, wherein benzylamine and halogenatedethyl acetate are taken, and are subjected to a room temperature stirring reaction in an organic solvent, water is added after the HPLC detection results show that the reaction is completed, extracting is performed, an organic mixed solution of hydrochloric acid is added into the organic layer in a dropwise manner, the pH value is adjusted to 1-2, the solid is precipitated, and filtering and drying are performed; and adding water into the N-benzyl glycine ethyl ester hydrochloride, carrying out stirring dissolving, adjusting the pH value to 7-8 by using an alkali, adding an organic solvent, extracting, drying the organic layer by using anhydrous sodium sulfate, filtering, and carrying out pressure reducing concentrating to achieve a dry state so as to obtain the product N-benzyl glycine ethyl ester hydrochloride. The preparation method of the invention is simple in process operation, high in product yield, high in product purity and easy for industrial production.
Selective Functionalization of Aliphatic Amines via Myoglobin-Catalyzed Carbene N-H Insertion
Fasan, Rudi,Sreenilayam, Gopeekrishnan,Steck, Viktoria
, p. 224 - 229 (2020/02/15)
Engineered myoglobins have recently gained attention for their ability to catalyze a variety of abiological carbene transfer reactions including the functionalization of amines via carbene insertion into N-H bonds. However, the scope of myoglobin and other hemoprotein-based biocatalysts in the context of this transformation has been largely limited to aniline derivatives as the amine substrates and ethyl diazoacetate as the carbene donor reagent. In this report, we describe the development of an engineered myoglobin-based catalyst that is useful for promoting carbene N-H insertion reactions across a broad range of substituted benzylamines and α-diazo acetates with high efficiency (82-99percent conversion), elevated catalytic turnovers (up to 7,000), and excellent chemoselectivity for the desired single insertion product (up to 99percent). The scope of this transformation could be extended to cyclic aliphatic amines. These studies expand the biocatalytic toolbox available for the selective formation of C-N bonds, which are ubiquitous in many natural and synthetic bioactive compounds.
