76103-96-3Relevant academic research and scientific papers
Enantioselective decarboxylative Mannich reaction of β-keto acids withC-alkynylN-BocN,O-acetals: access to chiral β-keto propargylamines
Chen, Li-Jun,Li, Wei,Shen, Bao-Chun,Sun, Zhong-Wen,Xie, Hui-Ding,Zhang, Cong-Cong
, p. 8607 - 8612 (2021/10/20)
The chiral keto-substituted propargylamines are an essential class of multifunctional compounds in the field of organic and pharmaceutical synthesis and have attracted considerable attention, but the related synthetic approaches remain limited. Therefore, a concise and efficient method for the enantioselective synthesis of β-keto propargylaminesviachiral phosphoric acid-catalyzed asymmetric Mannich reaction between β-keto acids andC-alkynylN-BocN,O-acetals as easily availableC-alkynyl imine precursors has been demonstrated here, affording a broad scope of β-ketoN-Boc-propargylamines in high yields (up to 97%) with generally high enantioselectivities (up to 97?:?3 er).
Enaminone amides as novel orally active GABAA receptor modulators
Hogenkamp, Derk J.,Johnstone, Timothy B. C.,Huang, Jin-Cheng,Li, Wen-Yen,Tran, Minhtam,Whittemore, Edward R.,Bagnera, Rudy E.,Gee, Kelvin W.
, p. 3369 - 3379 (2008/02/09)
A series of enaminone esters and amides have been developed as potent allosteric modulators of γ-aminobutyric acidA (GABA A) receptors. The compounds bind to a novel modulatory site that is independent of the benzodiazepine (BZ), isosteric GABA, and neuroactive steroid binding sites. Structure-activity relationship (SAR) studies resulted in the synthesis of the c-Bu amide 16h with an in vitro potency of 7 nM based on inhibition of [35S]TBPS binding. The activity of the enaminones as positive allosteric modulators was confirmed with electrophysiological measurements in oocytes expressing α1β2γ 2L GABAA receptors. The i-Pr, s-Bu, c-Pr, and c-Bu amides (16e-h) were orally active in mice with profound central nervous system depressant effects. The i-Pr amide 16e was an orally active anxiolytic in the mouse light-dark paradigm.
2-Substituted-4-aryl-5-thiazolecarboxylic acids and their derivatives as safening agents
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, (2008/06/13)
These compounds have been found to be effective in reducing herbicidal injury to direct-seeded rice caused by 2-chloro-2',6'-diethyl-N-(butoxymethyl)acetanilide.
