173064-91-0

Upstream product

• 5436-21-5 acetylacetaldehyde dimethyl acetal 
• 28566-12-3 3-amino-cyclopent-2-en-1-one 
• 853179-76-7 methyl 2-((E)-2-(methoxycarbonyl)vinyl)-6-methylpiridine-3-carboxylate 
• 38116-61-9 2-hydroxy-6-methylnicotinic acid 
• 885277-48-5 methyl 2-bromo-6-methylpyridine-3-carboxylate 
• 3859-41-4 1,3-cyclopentadione 
• 78-94-4 methyl vinyl ketone 
• 853179-88-1 methyl 2-(2-(methoxycarbonyl)ethyl)-6-methylpyridine-3-carboxylate 

Relevant academic research and scientific papers

PROTEIN TYROSINE PHOSPHATASE INHIBITORS

Compounds of Formula la or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases in the view of their ability to inhibit SHP2. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

PROTEIN TYROSINE PHOSPHATASE INHIBITORS

Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

GHRELIN O-ACYLTRANSFERASE INHIBITORS

This invention relates to novel compounds according to Formula (I) which are inhibitors of ghrelin O-acyltransferase (GOAT), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment

Metal-free michael-addition-initiated three-component reaction for the regioselective synthesis of highly functionalized pyridines: Scope, mechanistic investigations and applications

A metal-free and completely regioselective three-component synthesis of highly functionalized pyridines from 1,3-dicarbonyl derivatives and Michael acceptors has been achieved. Activated Michael acceptors, that is, β,γ-unsaturated α-oxo carbonyl derivatives, were utilized, allowing substitution at the 4-position and remarkable functional diversity at the 2-position of the pyridine ring. The scope and limitations of this environmentally friendly domino reaction are disclosed, with full experimental data, and the results of mechanistic investigations are discussed. The three-component synthesis of polysubstituted pyridines starting from 1,3-dicarbonyl compounds, α,β-unsaturated carbonyl derivatives and ammonium acetate has been studied, including the scope and mechanism. This methodology is a rare example of a totally regioselective multicomponent access to highly substituted pyridines that complies with many of the stringent criteria of sustainable chemistry. Copyright

Efficient and fast Heck vinylation of 2-bromo-6-methyl pyridines with methylacrylate. Application to the synthesis of 6-methyl cyclopenta[b]pyridinone

Heck vinylation of 2-bromo-6-methyl-3-substituted pyridines using η3-allylpalladium chloride dimer/P(o-Tol)3 complex/toluene and dimethylacetamide (DMA) as co-solvent with methyl acrylate is reported. Electronic and steric effects were investigated engaging diversely 2-bromo-3,6-disubstituted pyridines. As application, a new synthesis of the 6-methyl cyclopenta[b]pyridinone building-block connecting Heck vinylation, alkene reduction and Dieckmann condensation is described.

A regioselective synthesis of 4-methyl-1-pyrindan-5-one

The enamine 7 reacts with crotonic aldehyde in the presence of p-toluenesulphonic acid via the intermediate 8 to yield regioselectively the unknown title compound 9. In alkaline medium, 9 is also formed from 7 and acetylacetaldehyde dimethyl acetal as well as small amounts of 11 and 12; under acidic conditions, however, mixtures of the regioisomers 9/9a are obtained in poor yield. 9a can be separated by fractional crystallisation of the hydrochlorides. Corresponding to 7 the homologous enamine 13 and acetylacetaldehyde acetal by alkaline catalysis gives the 4-methyltetrahydroquinolinone 1, respectively. Improved experimental details for an efficient preparation of the starting compounds 3 and 4 are given.