67808-34-8

Upstream product

• 1003-31-2 thiophene-2-carbonitrile 
• 74-88-4 methyl iodide 
• 4565-31-5 5-formyl-2-thiophencarboxylic acid 
• 133380-60-6 methyl 5-((hydroxyimino)methyl)thiophene-2-carboxylate 
• 50340-79-9 thiophene-2,5-dicarboxylic acid monomethyl ester 
• 1206087-41-3 methyl 5-carbamoyl-2-thiophenecarboxylate 
• 67808-64-4 5-formyl-thiophene-2-carboxylic acid methyl ester 

Downstream Products

• 133380-65-1 5-(5-phenyl-1,2,4-oxadiazol-3-yl)-2-thiophenecarboxylic acid 
• 133380-93-5 methyl 5-(5-phenyl-1,2,4-oxadiazol-3-yl)-2-thiophenecarboxylate 

Relevant academic research and scientific papers

Ag(I)-Catalyzed C-H Carboxylation of Thiophene Derivatives

CO2utilization is an attractive aspect as it allows the direct conversion of CO2into valuable chemicals. In this regard, direct incorporation of CO2into the C-H bond of heteroaromatic compounds is important due to the ubiquitous structural motifs of the heteroaromatic carboxylic acids. Herein, we report the Ag-catalyzed C-H carboxylation of thiophene derivatives. This new catalytic system involving a phosphine ligand and lithiumtert-butoxide enables the direct carboxylation of thiophenes under mild reaction conditions. Experimental studies revealed that the use oftert-butyl alkoxide is critical for the exergonic formation of an arylsilver intermediate, and the results were further supported by density functional theory calculations.

COMPOUNDS AND METHODS for the inhibition of HDAC

Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.

Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F

A series of dipeptide nitriles with different P3 substituents was designed to explore the S3 binding pocket of cathepsin S. Racemic 7-16 and the enantiopure derivative (R)-22 proved to be potent inhibitors of human cathepsin S and exhibited notable selectivity over human cathepsins L, K, and B. Inhibition of cathepsin F, the functional synergist of cathepsin S, was not observed. The azadipeptide analogue of 22, compound 26, was highly potent but nonselective.

Pyrimidine derivatives

The object of the invention is to provide a novel compound having an inhibitory action on PDE4 activity with fewer side effects. The invention provides a compound represented by the following general formula (1), possible stereoisomers thereof or racemate

PYRIMIDINE DERIVATIVE

A compound represented by the general formula (1) which has an inhibitory effect on PDE4 activity and produces little adverse side effects: wherein Ar1 represents a furyl, thienyl, triazolyl, thiazolyl, oxazolyl or benzothiazolyl group; Ar2 represents -E-AR21-G-Q (where Ar21 represents a benzene or naphthalene ring; E represents a single bond or an alkylene group; G represents a single bond, an alkylene group or an alkenylene group; and Q represents a carboxyl group, -CON(R41)(R42) or -COOR43), -E-Ar21-G2-G-Q (where E, Ar21, G and Q are as defined above; and G2 represents -O-, -S-, -SO-, -SO2- or -NRG21-) or a monocyclic aromatic heterocyclic ring other than a pyrazolyl group; R1 and R2 are the same as or different from each other and independently represent a hydrogen atom, an alkyl group which may be substituted or the like; and R3 represents a hydrogen atom or an alkyl group which may be substituted.

3-SUBSTITUTED-2-OXINDOLE DERIVATIVES

This invention relates to novel 3-substituted-2-oxindole derivatives which are inhibitors of prostaglandin H 2 synthase, 5-lipoxygenase and interleukin-1 biosynthesis. The compounds of the invention are useful as inhibitors of prostaglandin H 2 synthase and interleukin-1 biosynthesis, per se, and as analgesic, antiinflammatory and antiarthritic agents in the treatment of chronic inflammatory diseases. This invention also relates to pharmaceutical compositions comprising said 3-substituted-2-oxindole derivatives; to methods of inhibiting prostaglandin H 2 synthase and biosynthesis of interleukin-1; and to treating chronic inflammatory diseases in a mammal with said compounds. Further, this invention relates to certain novel carboxylic acids useful as intermediates in the preparation of the 3-substituted-2-oxindole derivatives of this invention and to a process for the preparation of the 3-substituted-2-oxindole derivatives.