32986-65-5

Upstream product

• 500-22-1 3-pyridinecarboxaldehyde 
• 91076-37-8 trimethylsilylacetaldehyde tert-butylimine 
• 1291078-55-1 (E)-2-[2-(pyridin-3-yl)ethenyl]-1,3-dioxolane 
• 1120-90-7 3-iodopyridine 
• 107-18-6 allyl alcohol 
• 6628-07-5 N-allyl-N-methylaniline 
• 626-55-1 3-Bromopyridine 
• 3054-95-3 acrylaldehyde diethyl acetal 
• 59607-99-7 ethyl (E)-3-(pyridin-3-yl)acrylate 
• 100-55-0 3-hydroxymethylpyridin 
• 120277-39-6 trans-3-(pyridin-3-yl)-allyl alcohol 
• 2136-75-6 (triphenylphosphoranylidene)acetaldehyde 
• 75-07-0 acetaldehyde 
• 1802-16-0 3-(3-pyridinyl)propionaldehyde 

Downstream Products

• 1251832-94-6 1-(methoxy(pyridin-3-yl)methyl)-5-phenylpyrazolo[5,1-a]isoquinoline 
• 54356-27-3 (E)-3-(pyridin-3-yl)acrylonitrile 
• 83665-87-6 (E)-3-(pyridin-3-yl)prop-2-en-1-amine 
• 98-86-2 acetophenone 
• 1513846-31-5 diethyl ((2S,3S)-5-oxo-2-phenyl-3-(pyridin-3-yl)tetrahydrofuran-2-yl)phosphonate 
• 1357468-57-5 N-benzyl-2-ethyl-3-(3-pyridyl)pyrrole 
• 1357468-45-1 N-benzyl-3-ethyl-3-(3-pyridyl)-1,3-dihydropyrrol-2-one 
• 1357468-58-6 2-ethyl-N-phenyl-3-(3-pyridyl)pyrrole 
• 1357468-47-3 3-ethyl-3-(3-pyridyl)-N-phenyl-1,3-dihydropyrrol-2-one 

Relevant academic research and scientific papers

Iron-Catalyzed ?±,?-Dehydrogenation of Carbonyl Compounds

An iron-catalyzed α,β-dehydrogenation of carbonyl compounds was developed. A broad spectrum of carbonyls or analogues, such as aldehyde, ketone, lactone, lactam, amine, and alcohol, could be converted to their α,β-unsaturated counterparts in a simple one-step reaction with high yields.

RIPK1 INHIBITORS AND METHODS OF USE

The invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I) compounds act as RIPK1 inhibitors and may be useful in preventing, treating, or acting as a therapeutic agent against, diseases associated with RIPK1.

Formation of Polycyclic Skeletons by Photochemical Transformations of Pyridyl- and Thienylbutadiene Derivatives

In order to study the influence of heterocyclic nuclei on the photochemical behavior of conjugated butadiene systems, novel butadiene derivatives E,Z- and E,E-2/3-[4-(2-vinylphenyl)buta-1,3-dienyl]thiophene as well as E,Z- and E,E-3/4-[4-(2-vinylphenyl)buta-1,3-dienyl]pyridine have been synthesized. The Wittig reaction was utilized in a two-step reaction course. During the first Wittig reaction, the corresponding aldehydes, namely 2/3-thiophenecarboxaldehyde and 3/4-pyridinecarboxaldehyde, reacted with formylmethylenetriphenylphosphorane to give the corresponding acrylaldehydes, which reacted with the diphosphonium salt of α,α′-o-xylenedibromide in the second Wittig reaction to give new butadiene derivatives. These butadiene derivatives afforded, by photochemical intramolecular cycloaddition, new fused tricyclic as well as tetracyclic derivatives. For the first time, a study of efficiency was conducted where the efficiency of intramolecular cycloaddition of these heterocyclic butadiene derivatives was investigated by simultaneous use of ferrioxalate and valerophenone actinometers.

HETEROCYCLIC AMIDES AS KINASE INHIBITORS

Disclosed are compounds having the formula: (I) wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

Design, synthesis, and biological evaluation of 1,9-diheteroarylnona-1,3,6,8-tetraen-5-ones as a new class of anti-prostate cancer agents

In search of more effective chemotherapeutics for the treatment of castration-resistant prostate cancer and inspired by curcumin analogues, twenty five (1E,3E,6E,8E)-1,9-diarylnona-1,3,6,8-tetraen-5-ones bearing two identical terminal heteroaromatic rings have been successfully synthesized through Wittig reaction followed by Horner–Wadsworth–Emmons reaction. Twenty-three of them are new compounds. The WST-1 cell proliferation assay was employed to assess their anti-proliferative effects toward both androgen-sensitive and androgen-insensitive human prostate cancer cell lines. Eighteen out of twenty-five synthesized compounds possess significantly improved potency as compared with curcumin. The optimal compound, 78, is 14- to 23-fold more potent than curcumin in inhibiting prostate cancer cell proliferation. It can be concluded from our data that 1,9-diarylnona-1,3,6,8-tetraen-5-one can serve as a new potential scaffold for the development of anti-prostate cancer agents and that pyridine-4-yls and quinolin-4-yl act as optimal heteroaromatic rings for the enhanced potency of this scaffold. Two of the most potent compounds, 68 and 75, effectively suppress PC-3 cell proliferation by activating cell apoptosis and by arresting cell cycle in the G0/G1phase.

Structure-Activity Relationship Study of Heterocyclic Phenylethenyl and Pyridinylethenyl Derivatives as Tau-Imaging Agents That Selectively Detect Neurofibrillary Tangles in Alzheimers Disease Brains

In order to explore novel tau-imaging agents that can selectively detect neurofibrillary tangles in Alzheimers disease (AD) brains, we designed and synthesized a series of heterocyclic phenylethenyl and (3-pyridinyl)ethenyl derivatives with or without a dimethyl amino group. In in vitro autoradiography using AD brain sections, all radioiodinated ligands with a dimethyl amino group bound to Aβ deposits in the sections. In contrast, the ligands without a dimethyl amino group showed different patterns of radioactivity accumulation in the sections depending on the kind of heterocycle contained in their molecules. Particularly, a phenylethenyl benzimidazole derivative ([125I]64) showed marked radioactivity accumulation in the temporal lobe which corresponded with the distribution of tau deposits. [125I]64 also showed the most favorable pharmacokinetics in normal mouse brains (3.69 and 0.06% ID/g at 2 and 60 min postinjection, respectively) among all ligands in this study. Taken together, these results suggest that [123I]64 may be a new candidate tau-imaging agent.

Direct oxidative conversion of 3-aryl propionaldehydes to 3-aryl acroleins promoted by SOMO catalysis

A new direct oxidative transformation of 3-aryl propionaldehydes to 3-aryl acroleins promoted by SOMO catalysis has been realized with high efficiency under mild reaction conditions.

Pd-catalyzed cascade Heck-Saegusa: Direct synthesis of enals from aryl iodides and allyl alcohol

A new efficient Pd-catalyzed cascade Heck-Saegusa protocol for the synthesis of synthetically useful α,β-unsaturated aldehydes in high yields from readily available aryl iodides and allyl alcohol has been developed.

Palladium-catalyzed oxidative tandem reaction of allylamines with aryl halides leading to α,β-unsaturated aldehydes

A novel tandem protocol involving a Heck reaction process for the synthesis of α,β-unsaturated aldehydes has been developed. In the presence of Pd(OAc), PPh3, NaOAc, TBAB and air, N-allylbenzenamines underwent the reaction with various aryl hal

Acrolein diethyl acetal: A three-carbon homologating reagent for the synthesis of β-arylpropanoates and cinnamaldehydes by heck reaction catalyzed by a Kaiser oxime resin derived palladacycle

A polymer palladacycle derived from Kaiser oxime resin was used as a source of palladium(0) in the chemoselective Heck reaction of acrolein diethyl acetal with aryl halides under ligand-free conditions. The use of typical Heck conditions afforded 3-arylpropionic esters, and the process can be directed to the synthesis of cinnamaldehydes under Cacchi conditions. These processes take place with rather low loading of the catalyst, which can be recovered by simple filtration and reused for at least five runs without competitive dehalogenation. This is the first time that a supported palladium complex has been reused under Cacchi conditions. ICP-OES analyses of the Pd content of the crude products in both transformations indicated lower leaching for the esters than for the aldehydes in the range up to 0.08 ppm for the esters and 0.8 ppm for the aldehydes. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.