882029-94-9

Upstream product

• 882029-85-8 toluene-4-sulfonic acid 3-benzoyl-5-bromo-pyridin-2-yl ester 
• 98-88-4 benzoyl chloride 
• 1186608-72-9 5-bromo-3-phenyl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[3,4-b]pyridine 
• 875781-19-4 5-bromo-3-iodo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-pyrazolo[3,4-b]pyridine 
• 98-80-6 phenylboronic acid 
• 875781-18-3 5-bromo-3-iodo-1H-pyrazolo[3,4-b]pyridine 
• 875781-17-2 5-bromo-7-azaindazole 
• 875781-15-0 5-bromo-2-fluoro-3-pyridinecarboxaldehyde 
• 13472-81-6 3,5-dibromo-2-hydroxypyridine 
• 882029-80-3 p-toluenesulfonic acid 3,5-dibromo(pyridin-2-yl) ester 

Relevant academic research and scientific papers

Azaindazole bipyridine derivative myeloid cell proliferation inhibitor as well as preparation method and application thereof in pharmacy

The invention provides an azaindazole bipyridine derivative myeloid cell proliferation inhibitor shown as a formula I, wherein R1, R2 and R3 have the meanings defined in the specification of the invention. A compound in formula I can significantly inhibit proliferation and related disordersof myeloid cells represented by MOLM-16, HL-60, and MV-4-11. The formula I or salt thereof or the related pharmaceutical composition provided by the invention has excellent in-vivo and in-vitro inhibitory activity, good druggability, high bioavailability and no obvious damage to organs. Therefore, the compound shown in the formula I or the salt thereof and the related drug combination have huge clinical application prospects.

Synthesis of novel 1H-Pyrazolo[3,4-b]pyridine derivatives as DYRK 1A/1B inhibitors

As DYRK1A and 1B inhibitors, 1H-pyrazolo[3,4-b]pyridine derivatives were synthesized. Mostly, 3-aryl-5-arylamino compounds (6) and 3,5-diaryl compounds (8 and 9) were prepared and especially, 3,5-diaryl compound 8 and 9 showed excellent DYRK1B inhibitory enzymatic activities with IC50 Values of 3–287 nM. Among them, 3-(4-hydroxyphenyl), 5-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-b]pyridine (8h) exhibited the highest inhibitory enzymatic activity (IC50 = 3 nM) and cell proliferation inhibitory activity (IC50 = 1.6 μM) towards HCT116 colon cancer cells. Also compound 8h has excellent inhibitory activities in patient-derived colon cancer organoids model as well as in 3D spheroid assay model of SW480 and SW620. The docking study supported that we confirmed that compound 8h binds to DYRK1B through various hydrogen bonding interactions and hydrophobic interactions.

Regioselective functionalization of trisubstituted pyridines using a bromine-magnesium exchange

A tosyloxy substituent in position 2 allows a highly regioselective Br/Mg exchange reaction on 3,5-dibromopyridine derivatives using iso- PrMgCl·LiCl. The resulting functionalized pyridylmagnesium reagents react with various electrophiles in position 3. A

2-OXO-1-PYRROLIDINE DERIVATIVES

The present invention concerns 2-oxo-1 -pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.