34839-13-9Relevant articles and documents
Synthesis and in vitro antibacterial activity of novel fluoroalkyl-substituted pyrazolyl oxazolidinones
Yan, Lili,Wu, Jingjing,Chen, Heng,Zhang, Shaowu,Wang, Zhi,Wang, Hui,Wu, Fanhong
, p. 73660 - 73669 (2015)
A series of novel oxazolidinone derivatives bearing fluoroalkyl-substituted pyrazole as the C-ring structure were designed, synthesized and evaluated for their antibacterial activity against six Gram-positive bacterial pathogens. Most of the target compounds have good antibacterial activity. Especially, compounds 13f, 13i and 13l show excellent activity comparable to linezolid.
Lewis Acid-Catalyzed Addition of Benzophenone Imine to Epoxides Enables the Selective Synthesis and Derivatization of Primary 1,2-Amino Alcohols
Leitch, David C.,Lim, John Jin
, p. 641 - 649 (2018/05/14)
Benzophenone imine was found to be an effective ammonia surrogate for the selective preparation of primary 1,2-amino alcohols from epoxides, including enantiopure epichlorohydrin, in the presence of catalytic Y(OTf)3. High-throughput screening of 48 Lewis acids quickly identified Y(OTf)3 as an effective mediator of the addition reaction under mild conditions. Following acidic hydrolysis, the primary amino alcohol salt is revealed and partitions into the aqueous solution, while the benzophenone byproduct is easily removed by simple extraction with ethyl acetate. These ammonium salts can be directly Boc-protected or further derivatized without isolation to form benzamides and sulfonamides under Schotten-Baumann-type conditions in up to 79% isolated yield over three steps. This methodology has been used to prepare key intermediates for the synthesis of PRMT5 inhibitors with high enantiopurity as well as numerous other amide and sulfonamide derivatives.
A more than the penem matching bends down the ester side chain new synthetic method
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Paragraph 0028, (2017/08/25)
The invention discloses a novel synthetic method of a tebipenem pivoxil side chain. The method employs cheap and easily available raw material, has simple experimental operations, high overall yield and is applicable to industrialized production.