2057-32-1

Upstream product

• 56336-90-4 3-(2-pyridyl)propanal diethylacetal 
• 100-69-6 2-vinylpyridine 
• 201230-82-2 carbon monoxide 
• 2859-68-9 3-(pyridin-2-yl)-propanol 
• 109-06-8 α-picoline 
• 1749-29-7 2-pyridylmethyllithium 
• 2032-35-1 Bromoacetaldehyde diethyl acetal 
• 20461-86-3 2,2-diethoxy acetic acid 

Downstream Products

• 699021-09-5 2-{2-[4-(toluene-4-sulfonyl)-4,5-dihydrooxazol-5-yl]ethyl}pyridine 
• 311779-51-8 3⁽⁵⁾-(4-fluorophenyl)-5⁽³⁾-[1-hydroxy-3-(2-pyridyl)propyl]-4-(4-pyridyl)-pyrazole 
• 28819-26-3 methyl 3-(pyridin-2-yl)propanoate 
• 856858-86-1 2-amino-4-[2]pyridyl-butyric acid 
• 1381774-06-6 (S)-3-((S)-1-hydroxy-3-(pyridin-2-yl)propyl)-1-(4-methoxyphenyl)pyrrolidine-2-thione 
• 15197-75-8 3-(pyridin-2-yl)propanoic acid 
• 2859-68-9 3-(pyridin-2-yl)-propanol 

Relevant academic research and scientific papers

ECTONUCLEOTIDE PYROPHOSPHATASE/PHOSPHODIESTERASE 1 (ENPP1) MODULATORS AND USES THEREOF

Provided herein are small molecule modulators of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Chemo- and Regioselective Organo-Photoredox Catalyzed Hydroformylation of Styrenes via a Radical Pathway

An unprecedented, chemo- and regioselective, organo-photoredox catalyzed hydroformylation reaction of aryl olefins with diethoxyacetic acid as the formylation reagent is described. In contrast to traditional transition metal promoted ionic hydroformylation reactions, the new process follows a unique photoredox promoted, free radical pathway. In this process, a formyl radical equivalent, produced from diethoxacetic acid through a dye (4CzIPN) photocatalyzed, sequential oxidation-decarboxylation route, regio- and chemoselectively adds to a styrene substrate. Importantly, under the optimized reaction conditions the benzylic radical formed in this manner is reduced by SET from the anion radical of 4CzIPN to generate a benzylic anion. Finally, protonation produces the hydroformylation product. By using the new protocol, aldehydes can be generated regioselectively in up to 90% yield. A broad array of functional groups is tolerated in the process, which takes place under mild, metal-free conditions.

Chroman-4-one- and chromone-based sirtuin 2 inhibitors with antiproliferative properties in cancer cells

Sirtuins (SIRTs) catalyze the NAD+-dependent deacetylation of Nε-acetyl lysines on various protein substrates. SIRTs are interesting drug targets as they are considered to be related to important pathologies such as inflammation and aging-associated diseases. We have previously shown that chroman-4-ones act as potent and selective inhibitors of SIRT2. Herein we report novel chroman-4-one and chromone-based SIRT2 inhibitors containing various heterofunctionalities to improve pharmacokinetic properties. The compounds retained both high SIRT2 selectivity and potent inhibitory activity. Two compounds were tested for their antiproliferative effects in breast cancer (MCF-7) and lung carcinoma (A549) cell lines. Both compounds showed antiproliferative effects correlating with their SIRT2 inhibition potency. They also increased the acetylation level of α-tubulin, indicating that SIRT2 is likely to be the target in cancer cells. A binding mode of the inhibitors that is consistent with the SAR data was proposed based on a homology model of SIRT2.

Continuous-flow aerobic oxidation of primary alcohols with a copper(I)/TEMPO catalyst

A scalable, continuous-flow process has been developed to implement a homogeneous CuI/TEMPO catalyst system for aerobic oxidation of primary alcohols to aldehydes. This catalyst system is compatible with a wide range of alcohols bearing diverse functional groups. A dilute oxygen source (9% O2 in N2) is used to avoid flammable oxygen/organic mixtures. Residence times in the heated reaction zone can be as low as 5 min with activated (e.g., benzylic) alcohols. The method has been demonstrated with nine different alcohols, including one up to 100 g scale. This flow-based catalytic method exhibits significant advantages for aerobic oxidation of alcohols, including substantially shorter residence times and broader substrate scope relative to a Pd-catalyzed method that we reported recently.

Development of rationally designed DNA N6 adenine methyltransferase inhibitors

A series of bisubstrate inhibitors for DNA N6 adenine methyltransferase (Dam) have been synthesized by linking an amine analogue of S-adenosylmethionine to an aryl moiety designed to probe the binding pocket of the DNA adenine base. An initial structure-activity relationship study has identified substituents that increase inhibitor potency to the ～10 μM range and improve selectivity against the human cytosine methyltransferase Dnmt1.

Highly practical copper(I)/TEMPO catalyst system for chemoselective aerobic oxidation of primary alcohols

Aerobic oxidation reactions have been the focus of considerable attention, but their use in mainstream organic chemistry has been constrained by limitations in their synthetic scope and by practical factors, such as the use of pure O2 as the oxidant or complex catalyst synthesis. Here, we report a new (bpy)CuI/TEMPO catalyst system that enables efficient and selective aerobic oxidation of a broad range of primary alcohols, including allylic, benzylic, and aliphatic derivatives, to the corresponding aldehydes using readily available reagents, at room temperature with ambient air as the oxidant. The catalyst system is compatible with a wide range of functional groups and the high selectivity for 1° alcohols enables selective oxidation of diols that lack protecting groups.

HETEROARYL SUBSTITUTED THIENO[2,3-D]PYRIMIDINE AND THEIR USE AS ADENOSINE A2A RECEPTOR ANTAGONISTS

This invention relates to a novel thieno[2,3-d]pyrimidine, Z, and its therapeutic and prophylactic uses, wherein X, R1 and R2 are defined in the specification. Disorders treated and/or prevented include Parkinson's Disease.

2-(Aminomethyl)-5-Chlorobenzylamide Derivatives and their use as Inhibitors of the Clotting Factor Xa

The invention relates to 2-(aminomethyl)-5-chlorobenzylamide derivatives and their use as inhibitors of coagulation factor Xa. The compounds are suitable for the treatment and prophylaxis of cardiovascular and thrombotic events.

SUBSTITUTED PIPERAZINE CARBAMATES FOR USE AS INHIBITORS OF HORMONE SENSITIVE LIPASE

Novel substituted piperazine carbamates of formula (I), pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are usef