19745-72-3Relevant articles and documents
Synthetic method for tyramine hydrochloride
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Paragraph 0030; 0031; 0032, (2017/01/31)
The invention discloses a synthetic method for tyramine hydrochloride. The synthetic method includes the steps that phenol is used as a raw material and reacts with aminoacetonitrile to generate p-hydroxy phenylaminoethanol, p-hydroxy phenylaminoethanol is subjected to catalytic reduction to obtain tyramine hydrochloride, activated carbon and copper powder are used as a composite catalyst, and the mass ratio of the activated carbon to the copper powder is (3-5):1. As the activated carbon and copper powder composite catalyst is added, the ratio of the dosage of the catalyst to the substrate weight can be reduced to (0.1-0.2):1. The catalytic efficiency is improved remarkably, the number of times of continuously using the catalyst can be increased to be 10 or more, the total yield of the reactions is increased, and the synthetic method has high economic benefits.
4-Hydroxyphenacyl Ammonium Salts: A Photoremovable Protecting Group for Amines in Aqueous Solutions
Bownik, Iwona,?ebej, Peter,Literák, Jaromír,Heger, Dominik,?imek, Zdeněk,Givens, Richard S.,Klán, Petr
, p. 9713 - 9721 (2015/10/12)
Irradiation of N-protected p-hydroxyphenacyl (pHP) ammonium caged derivatives at 313 nm releases primary and secondary amines or ammonia in nearly quantitative yields via the photo-Favorskii reaction when conducted in acidic or neutral aqueous buffered media. The reaction efficiencies are strongly dependent on the pH with the most efficient and highest yields obtained when the pH of the media maintains the ammonium and p-hydroxyl groups as their conjugate acids. For example, the overall quantum yields of simple secondary amines release are 0.5 at acidic pH from 3.9 to 6.6 dropping to 0.1 at neutral pH 7.0 and 0.01 at pH 8.4. Speciation studies provide an acid-base profile that helps define the scope and limitations of the reaction. When the pKa of the ammonium group is lower than that of the phenolic hydroxyl group, as is the case for the α-amino-protected amino acids, the more acidic ammonium ion deprotonates as the media pH is changed from acidic toward neutral or basic, thus diminishing the leaving group ability of the amino group. This, in turn, lowers the propensity for the photo-Favorskii rearrangement reaction to occur and opens the reaction pathway to alternative competing photoreduction process.
Discovery and synthesis of a novel series of liver X receptor antagonists
Nian, Siyun,Gan, Xia,Tan, Xiangduan,Yu, Zhenpeng,Wang, Panfeng,Chen, Xing,Wang, Guoping
, p. 628 - 635 (2015/09/07)
Fourteen novel compounds were prepared and their antagonistic activities against liver X receptors (LXR) α/β were tested in vitro. Compound 26 had an IC50 value of 6.4 μM against LXRα and an IC50 value of 5.6 μM against LXRβ. Docking studies and the results of structure-activity relationships support the further development of this chemical series as LXRα/β antagonists.
Synthesis and biological evaluation of imidazol-2-one derivatives as potential antitumor agents
Xue, Na,Yang, Xiaochun,Wu, Rui,Chen, Jing,He, Qiaojun,Yang, Bo,Lu, Xiuyang,Hu, Yongzhou
, p. 2550 - 2557 (2008/09/21)
A new series of aryl substituted imidazol-2-one derivatives structurally related to combretastatin A-4 (CA-4) were synthesized and evaluated for their cytotoxic activities in vitro against various human cancer cell lines including MDR cell line. The cytotoxic effects of compounds 7b and 7i proved to be similar to or greater than that of docetaxel. The highly active compound 7b also exhibited excellent inhibitory activity on tumor growth in vivo.
