20890-12-4

Upstream product

• 1121-60-4 pyridine-2-carbaldehyde 
• 98-86-2 acetophenone 
• 20842-76-6 3-hydroxy-1-phenyl-3-(pyridin-2-yl)propan-1-one 
• 20913-05-7 (Benzoylmethylene)triphenylphosphorane 
• 3453-00-7 diethyl benzoylmethylphosphonate 
• 109-06-8 α-picoline 
• 1945-84-2 2-ethynylpyridine 
• 100-52-7 benzaldehyde 
• 611-73-4 Benzoylformic acid 
• 54495-51-1 (E)-3-(2-pyridyl)acrylic acid 
• 109-04-6 2-bromo-pyridine 
• 4187-87-5 1-Phenyl-2-propyn-1-ol 

Downstream Products

• 83426-01-1 (E)-1-Phenyl-3-pyrid-2-yl-propenon-methoiodid 
• 929600-75-9 3-(2-pyridyl)-4-nitro-1-phenyl-butan-1-one 
• 1224605-96-2 (R)-1-phenyl-3-(diphenylarsanyl)-3-(pyridin-2-yl)propanone 
• 56741-25-4 1-phenyl-3-(pyridin-2-yl)propan-1-one 

Relevant academic research and scientific papers

Organic base-mediated condensation of pyridinecarboxaldehydes to azachalcones

A DBU-mediated aldol condensation-dehydration sequence has been used to prepare a series of synthetically important substituted 2- and 3-azachalcones. Michael products that typically accompany this sequence with inorganic bases were not observed in this p

Enantioselective Michael addition of 2-nitropropane to chalcone analogues catalyzed by chiral azacrown ethers based on α-D-glucose and D-mannitol

The chiral monoaza-15-crown-5 type lariat ethers 1 and 2 derived from α-D-glucose and from D-mannitol, respectively, have been applied as phase transfer catalysts in the enantioselective Michael addition of 2-nitropropane to aromatic 3b-c and heteroaromatic 3d-h chalcone analogues. Among the catalysts, the glucose-based 1c with a phosphinoxidobutyl side arm proved to be the most effective, it inducing 34% e.e. for 4b, 59% e.e. for 4c, 80% e.e. for 4d, 64% e.e. for 4e, 17% e.e. for 4f. Catalyst 1a having 3-hydroxypropyl substituent resulted in 81% e.e. for compound 4g. The formation of the (+)-(S)-enantiomer of 4 was preferred using crown ethers 1a-c, while the (-)-(R)-enantiomer was in excess with catalyst 2. The absolute configuration of the Michael adduct 4d was determined by single-crystal X-ray analysis.

Copper-Mediated Cross-Dehydrogenative Coupling of 2-Methylpyridine and 8-Methylquinoline with Methyl Ketones and Benzamides

A synthetic method to prepare (E)-(pyridin-2-yl)enones and (E)-(quinolin-8-yl)enones that relies on the respective copper(I)-catalyzed formal cross-dehydrogenative coupling (CDC) reaction of 2-methylpyridine and 8-methylquinoline with methyl ketones has been discovered. The mechanism was delineated to follow a pathway involving oxidation of the N-heterocycle to its corresponding aldehyde adduct prior to reaction with the methyl ketone. The versatility and substrate dependent divergence in the reactivity of the copper-mediated CDC strategy was exemplified by its application to the synthesis of N-(quinolin-8-ylmethyl)amide and N-(quinolin-8-ylmethyl)aniline adducts on switching the cross-coupling partner to benzamides or an aniline derivative.

Activated hydrotalcites as catalysts for the synthesis of chalcones of pharmaceutical interest

The Claisen-Schmidt condensation between benzaldehyde and acetophenone has been carried out in the presence of calcined-rehydrated hydrotalcites as solid-base catalysts. The rehydration method and the effect of the water content as well as the chemical composition of the rehydrated Al-Mg mixed oxides have been studied. The results showed that an Al-Mg mixed oxide with an Al/(Al+Mg) molar ratio of 0.25 with a water content of 35 wt% was the optimum catalyst which gives excellent activity for this type of condensation. This optimized catalyst has been applied to the synthesis of several chalcones with antiinflammatory, antineoplasic, and diuretic pharmacological activities achieving in all cases excellent activity and selectivity to the corresponding chalcones. A comparative study in the homogeneous phase using KOH as base catalyst showed that the rehydrated Al-Mg mixed oxides can compete with the conventional KOH when the reaction is performed at higher reaction temperatures. This behavior is not attributed to a lower intrinsic activity of the active sites on the solid, but to the small concentration of accessible active sites existing on the rehydrated sample.

Design and biological evaluation of novel tubulin inhibitors as antimitotic agents using a pharmacophore binding model with tubulin

Although the structure has been elucidated for the binding of colchicine and podophyllotoxin as potent destabilizer for microtubule formation, very little is known about MDL-27048, a competitive inhibitor for colchicine and podophyllotoxin. The structural

Regiodivergent synthesis of vinyl trifluoromethansulfonates γ/δ lactones: Via 1,6 addition/intramolecular one-pot annulation of 1,4-dihidropyridines derivated from pyridinyl propenones

We report a novel intramolecular 1,6 oxa-Michael addition on substituted dihydropyridines to obtain 5 and 6 member ring lactones in an one-pot reaction starting from activated pyridinyl propenones, without organic catalysis or presence of bulky groups in

Cascade Reaction of α, β-Unsaturated Ketones and 2-Aminoaryl Alcohols for the Synthesis of 3-Acylquinolines by a Copper Nanocatalyst

3-Acylquinolines possess widespread applications in functional chemicals. However, the convenient and selective synthesis of such important substructures has to date remained a challenge. Herein, we report a method to access 3-acylquinolines from α, β-unsaturated ketones and 2-aminoaryl alcohols in one pot with a copper nanocatalyst supported on nitrogen-silica-doped carbon (Cu/N?SiO2?C). Mechanistically, the construction of the product involves a cascade procedure including radical-type oxidation of 2-aminoaryl alcohols, aza-Michael addition and annulation. This developed protocol proceeds with merits of mild reaction conditions, good functional group tolerance, earth-abundant and reusable copper catalyst, easily available stocks and O2 as the sole oxidant, which provides an alternative way for the sustainable synthesis of quinoline derivatives. (Figure presented.).

New sp3diphosphine-based rhodium catalysts for the asymmetric conjugate addition of aryl boronic acids to 3-azaarylpropenones

Different chiral diphosphine ligands were successfully applied to the rhodium catalyzed asymmetric conjugate addition of differently substituted boronic acids to 3-azaarylpropenones containing both pyridinyl and imidazolyl cores. Atropoisomeric (S)-TetraM

Unsaturated ketone compound as well as preparation method and application thereof

The present invention relates to a novel GPR52 antagonist. Specifically, the invention relates to an unsaturated ketone compound, a pharmaceutically acceptable salt, a stereoisomer or a prodrug molecule thereof, and a method for preparing a pharmaceutical composition thereof. The invention further relates to the use of the GPR52 antagonist as an orphan G protein coupled receptor GPR52 antagonist,and further relates to the use of the GPR52 antagonist in the preparation of drugs for preventing and treating Huntington's disease.

COMPOUNDS AND METHODS FOR TREATING OR PREVENTING HEART FAILURE

The present invention relates to the discovery of novel compounds that can be used to treat and/or prevent heart failure in a subject. In certain embodiments, the compounds of the invention are sulfide: quinone oxidoreductase (SQOR) inhibitors. In other e