110351-28-5Relevant academic research and scientific papers
A Br?nsted Acid Catalyzed Cascade Reaction for the Conversion of Indoles to α-(3-Indolyl) Ketones by Using 2-Benzyloxy Aldehydes
Banerjee, Ankush,Maji, Modhu Sudan
supporting information, p. 11521 - 11527 (2019/08/16)
A Br?nsted acid catalyzed, operationally simple, scalable route to several functionalized α-(3-indolyl) ketones has been developed and the long-standing regioisomeric issue has been eliminated by choosing appropriate carbonyls. A readily available and cheap bottle reagent was used as the catalyst. This protocol was also applicable to the synthesis of densely functionalized α-(3-pyrrolyl) ketones. A detailed mechanistic study confirmed the involvement of enolether as a reaction intermediate. Several postsynthetic modifications along with easy access to β-carboline, tryptamines, tryptophols, and spiro-indolenine proclaim the synthetic utility of this powerful building block. On the basis of this concept, functionalized carbazoles were constructed by a cascade annulation strategy.
Discovery of novel 20S proteasome inhibitors by rational topology-based scaffold hopping of bortezomib
Xu, Yulong,Yang, Xicheng,Chen, Yiyi,Chen, Hao,Sun, Huijiao,Li, Wei,Xie, Qiong,Yu, Linqian,Shao, Liming
supporting information, p. 2148 - 2152 (2018/05/25)
A series of structurally novel proteasome inhibitors 1–12 have been developed based rational topology-based scaffold hopping of bortezomib. Among these novel proteasome inhibitors, compound 10 represents an important advance due to the comparable proteasome-inhibitory activity (IC50 = 9.7 nM) to bortezomib (IC50 = 8.3 nM), the remarkably higher BEI and SEI values and the effectiveness in metabolic stability. Therefore, compound 10 provides an excellent lead suitable for further optimization.
Boric acid compound used as 20S proteasome inhibitor, and preparation method thereof
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Paragraph 0165; 0166; 0167, (2017/09/19)
The invention relates to the fields of pharmaceutical chemistry and medicine therapeutics, concretely relates to new boric acid compounds, and a preparation method and a use thereof, and especially relates to a boric acid compound used as a 20S proteasome inhibitor, and a preparation method thereof. The invention also discloses a boric acid compound represented by formula I, and a preparation method thereof. A result of bioactive screening test shows that the compound prepared in the invention has a proteasome inhibition function, and can be further used for preparing medicines for treating proteasome correlated diseases.
Synthesis of a regular 24-membered cyclodepsipeptide by direct amide cyclization
K?ttgen, Peter,Linden, Anthony,Heimgartner, Heinz
experimental part, p. 689 - 698 (2009/12/26)
Aminoisobutyric Acid, Crystal Structure The synthesis of a 24-membered cyclic depsipeptide with an alternating sequence of phenyllactic acid and α-aminoisobutyric acid (Aib) is described. The linear precursor was prepared via the 'azirine/oxazolone method
ENZYME-MEDIATED ASYMMETRIC HYDROLYSIS OF α-BENZYLOXYCARBOXYLIC ESTERS
Kato, Yasuo,Ohta, Hiromichi,Tsuchihashi, Gen-ichi
, p. 1303 - 1306 (2007/10/02)
Incubation of dl-α-benzyloxycarboxylic esters with grown cells of a bacterium, Corynebacterium equi IFO 3730, afforded the chiral esters of high optical purities via asymmetric hydrolysis.This reaction has been revealed to have a wide applicability to alkene- and arylalkene-carboxylic esters.
