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M Chen, A Suzuki, S Thakkar, K Yu, C Hu, W Tong. DILIrank:按人类发展药物诱导肝损伤风险排名的最大参考药物清单。《药物发现今日》2016, 21(4): 648-653. PMID:26948801 DOI:10.1016/j.drudis.2016.02.015
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Method for producing amines by homogeneously catalyzed reductive amination of carbonyl compounds
申请人:Riermeier Thomas
公开号:US06884887B1
公开(公告)日:2005-04-26
The invention relates to the preparation of chiral or achiral amines by reaction of aldehydes or ketones with ammonia or primary or secondary amines in the presence of hydrogen and in the presence of homogeneous metal catalysts under mild conditions. Metal catalysts which can be used are complexes of late transition metals with chiral or achiral phosphorus-containing ligands.
A series of benzimidazole derivatives, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
Scope and limitations of reductive amination catalyzed by half-sandwich iridium complexes under mild reaction conditions
作者:Dat P. Nguyen、Rudolph N. Sladek、Loi H. Do
DOI:10.1016/j.tetlet.2020.152196
日期:2020.8
broad assortment of carbonyl-containing compounds. In aqueousmedia, selective reduction of carbonyls to 1° amines was achieved in the absence of acids. Unfortunately, at Ir catalyst concentrations of <1 mM in water, reductive amination efficiency dropped significantly, which suggest that this catalytic methodology might be not suitable for aqueous applications where very low catalyst concentration is
使用甲酸铵作为氮源和氢化物源的半夹心铱配合物可以促进醛和酮向 1°胺的转化。为了优化这种绿色化学合成方法,我们在生理温度 (37 °C) 和环境压力下在常见极性溶剂中测试了各种羰基底物。我们发现,在甲醇中,对于广泛种类的含羰基化合物,可以实现胺对醇/酰胺产物的优异选择性。在水性介质中,在不存在酸的情况下,羰基化合物选择性还原为 1° 胺。不幸的是,在水中 Ir 催化剂浓度 <1 mM 时,还原胺化效率显着下降,
Acyloxymethyl Carbonochloridates. New Intermediates in Prodrug Synthesis
作者:Michael Folkmann、Frantz J. Lund
DOI:10.1055/s-1990-27124
日期:——
The synthesis of a number of stable acyloxymethyl carbonochloridates 7 has been accomplished in four steps from chloromethyl carbonochloridate 3. Each step has been optimized with propanoyloxymethyl carbonochloridate 7c as a model compound (64% overall yield). Diethyl ether-boron trifluoride catalyzes the conversion of carbonothioate 6cc to the carbonochloridate 7c by chlorination with sulfuryl chloride. Acylation of a few compounds containing hydroxy or amino groups by 7c is described.
Method of introducing amino group and method of synthesizing amino acid compound
申请人:——
公开号:US20040162434A1
公开(公告)日:2004-08-19
The present invention relates to a method for introducing an amino group into an organic acid or an organic ester by reacting an organic salt or an organic ester and ammonia under high-temperature and high-pressure water conditions, a method for synthesizing an amino acid or an amino ester by the above method, and a method for manufacturing an amino acid compound by synthesizing an amino acid or an amino ester by the above method and separating and refining it with an ion exchange resin.