23612-48-8Relevant articles and documents
A 2 - methyl -7 - aza indole synthesis method (by machine translation)
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Paragraph 0018-0052, (2019/10/29)
The invention discloses a 2 - methyl - 7 - aza indole synthesis method, comprises the following steps: the 2 - amino - 3 - chloro pyridine added in DMF, heating to 150 - 220 °C, adding Cp2 ZrCl2 And catalyst, under stirring conditions, adding methylacetylene, reflux reaction 4 - 6 h, after the reaction, filtration, the filtrate is distilled under reduced pressure to remove the DMF, ethyl acetate extraction, recrystallization, extraction, drying, to obtain 2 - methyl - 7 - azaindole. The application of the synthesis method adopts the one-pot synthesis, the operation is simple, without intermediate purification step, high conversion rate of raw materials, and has high economic benefits. (by machine translation)
Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity
De Vita, Elena,Schüler, Peter,Lovell, Scott,Lohbeck, Jasmin,Kullmann, Sven,Rabinovich, Eitan,Sananes, Amiram,He?ling, Bernd,Hamon, Veronique,Papo, Niv,Hess, Jochen,Tate, Edward W.,Gunkel, Nikolas,Miller, Aubry K.
, p. 8859 - 8874 (2018/10/09)
Kallikrein-related peptidase 6 (KLK6) is a secreted serine protease that belongs to the family of tissue kallikreins (KLKs). Many KLKs are investigated as potential biomarkers for cancer as well as therapeutic drug targets for a number of pathologies. KLK6, in particular, has been implicated in neurodegenerative diseases and cancer, but target validation has been hampered by a lack of selective inhibitors. This work introduces a class of depsipeptidic KLK6 inhibitors, discovered via high-throughput screening, which were found to function as substrate mimics that transiently acylate the catalytic serine of KLK6. Detailed structure-activity relationship studies, aided by in silico modeling, uncovered strict structural requirements for potency, stability, and acyl-enzyme complex half-life. An optimized scaffold, DKFZ-251, demonstrated good selectivity for KLK6 compared to other KLKs, and on-target activity in a cellular assay. Moreover, DKFZ-633, an inhibitor-derived activity-based probe, could be used to pull down active endogenous KLK6.
Asymmetric Hydrogenation of Azaindoles: Chemo- and Enantioselective Reduction of Fused Aromatic Ring Systems Consisting of Two Heteroarenes
Makida, Yusuke,Saita, Masahiro,Kuramoto, Takahiro,Ishizuka, Kentaro,Kuwano, Ryoichi
supporting information, p. 11859 - 11862 (2016/11/16)
High enantioselectivity was achieved for the hydrogenation of azaindoles by using the chiral catalyst, which was prepared from [Ru(η3-methallyl)2(cod)] and a trans-chelating bis(phosphine) ligand (PhTRAP). The dearomative reaction exclusively occurred on the five-membered ring, thus giving the corresponding azaindolines with up to 97:3 enantiomer ratio.