60317-41-1

Upstream product

• 3885-45-8 ethyl 2,3-dioxo-3-phenylpropanoate 
• 109-95-5 ethyl nitrite 
• 94-02-0 ethyl 3-oxo-3-phenylpropionate 
• 64-19-7 acetic acid 
• 7664-93-9 sulfuric acid 
• 81471-31-0 3-oxo-3-phenyl-propionimidic acid ethyl ester; hydrochloride 
• 98-86-2 acetophenone 
• 164661-67-0 ethyl (E)-2-hydroxyimino-3-oxo-3-phenylpropanoate 
• 70582-90-0 2-Benzoylacetimidsaeure-ethylester 

Downstream Products

• 6966-30-9 ethyl 2-acetamido-3-oxo-3-phenylpropanoate 
• 122088-81-7 2-benzamide-3-oxo-3-phenylpropionic acid ethyl ester 
• 854461-63-5 optically inactive 2-hydroxy-3-nitro-1,4-diphenyl-butane-1,4-dione 
• 3306-06-7 (1RS,2SR)-2-amino-1-phenyl-propane-1,3-diol 
• 15917-28-9 (2RS,3RS)-2-amino-3-hydroxy-3-phenyl-propionic acid ethyl ester 
• 90560-40-0 phenyllactic acid 
• 3651-13-6 5-methyl-3-phenyl-1H-pyrrole-2,4-dicarboxylic acid diethyl ester 
• 75-52-5 nitromethane 
• 64-17-5 ethanol 
• 119124-15-1 ethyl (Z)-2-methoxyimino-3-oxo-3-phenylpropanoate 
• 94709-11-2 2,3,4-trimethoxybenzophenone 
• 88854-18-6 (2RS,3RS)-3-acetoxy-2-acetylamino-3-phenyl-propionic acid ethyl ester 
• 21756-95-6 5-methyl-3-phenyl-1H-pyrrole-2-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

METHOD OF TREATING COCCIDIOIDES INFECTION

The invention relates to the therapeutic use of olorofim, 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide in the prevention and treatment of a fungal infection caused by a Coccidioides species.

Copper-Catalyzed Carbonyl Group Controlled Coupling of Isatin Oximes with Arylboronic Acids To Prepare N-Aryloxindole Nitrones

A variety of (E)-N-aryloxindole nitrones were prepared in good to excellent yields by using a copper-catalyzed coupling reaction of isatin oximes and arylboronic acids under mild conditions. Various arylboronic acids that contain sensitive functional groups were tolerated in the transformation, and detailed studies show that the carbonyl group of the isatin oximes serves as a ligand to control the formation of the (E)-oxindole nitrones. This method to prepare (E)-N-aryloxindole nitrones was easily performed on a gram scale and efficiently used to synthesize estrone-derived oxindole nitrone in high yield.

PHARMACEUTICAL FORMULATION

A pharmaceutical composition suitable for oral administration comprising particles of 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide is provided. Also provided is a pharmaceutical composition suitable for parenteral administration wherein the composition comprises 2-(1,5-dimethyl- 3-phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide. The compositions are useful in the treatment of fungal infection in a subject in need thereof.

Tandem C-N Bond Formation through Condensation and Metal-Free N-Arylation: Protocol for Synthesizing Diverse Functionalized Quinoxalines

Diverse functionalized quinoxalines were synthesized in good yields from arylamines and readily available β-keto oximes through condensation and metal-free N-arylation. The reaction was compatible with various functional groups, such as halides, cyano, and esters. A mechanism was proposed based on the experimental results. These quinoxalines were easily obtained on a gram scale and converted to various useful scaffolds. Compound LASSBio-1022 was prepared in 83% yield in two steps.

Rhodium-catalyzed asymmetric hydrogenation of tetrasubstituted β-acetoxy-α-enamido esters and efficient synthesis of droxidopa

A rhodium-catalyzed asymmetric hydrogenation of challenging tetrasubstituted β-acetoxy-α-enamido esters was developed, giving chiral β-acetoxy-α-amido esters in high yields with excellent enantioselectivities (up to >99% ee). The products could be easily transformed to β-hydroxy-α-amino acid derivatives which are valuable chiral building blocks and a novel route for the synthesis of droxidopa was also developed.

ANTIFUNGAL AGENTS

The invention provides a pyrrole compound, which compound is (a)2-(1,5-dimethyl-3- phenyl-1H-pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2- oxoacetamideor a deuterated derivative thereof, or(b)2-(1,5-dimethyl-3-phenyl-1H-pyrrol- 2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)-3-hydroxyphenyl)-2-oxoacetamide or a deuterated derivative thereof, or (c) a prodrug of compound (a) or a prodrug of compound (b), or a pharmaceutically acceptable salt or agriculturally acceptable salt of (a), (b) or (c). Also provided are combinations and compositions comprising the compound and known antifungal agents. The invention also relates to the therapeutic use of a compound of the invention in prevention or treatment of fungal diseases. It also relates to the use of:2-(1,5-dimethyl-3-phenyl-1H- pyrrol-2-yl)-N-(4-(4-(5-fluoropyrimidin-2-yl)piperazin-1-yl)phenyl)-2-oxoacetamide or an agriculturally acceptable salt thereof, or 2-(1,5-dimethyl-3-phenyl-1H-pyrrol-2-yl)-N-(4-(4- (5-fluoropyrimidin-2-yl)piperazin-1-yl)-3-hydroxyphenyl)-2-oxoacetamide or an agriculturally acceptable salt thereof, as an agricultural fungicide.

Biocatalytic Synthesis of Enantiopure β-Methoxy-β-arylalanine Derivatives

Chiral β-hydroxy-β-arylalanine and β-methoxy-β-arylalanine derivatives, which occur widely in marine nature products, were stereoselectively synthesized with 99 % ee values. The two erythro isomers were prepared by L- or D-aminoacylase-catalyzed resolution of the corresponding N-acetyl derivatives, whereas the two threo isomers were obtained only by D-aminoacylase-catalyzed resolution of the derivatives. erythro-β-Hydroxy-β-arylalanine derivatives were prepared by diastereoselective hydrogenation of ethyl 2-(hydroxyimino)-3-oxo-3-arylpropanoates, which were in turn acquired by the oximation of ethyl 3-oxo-3-arylpropanoates with ethyl nitrite in the presence of nano-K2CO3 with yields of 72 % to 80 %. β-Methoxy-β-arylalanine derivatives were synthesized through Williamson reactions between the corresponding β-hydroxy-β-arylalanines and iodomethane with silver oxide as base.

Further observations on conformational and substituent effects in acid-catalyzed "3 + 1" cyclizations of tripyrranes with aromatic dialdehydes

Tripyrranes with tert-butyl and phenyl substituents have been prepared and used to synthesize oxybenziporphyrins, oxypyriporphyrins, benzocarbaporphyrins, and azuliporphyrins with phenyl and tert-butyl substituents via a "3 + 1" methodology. The proton NM

PYRROLE ANTIFUNGAL AGENTS

The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.

Silica sulfuric acid/NaNO2 as a novel heterogeneous system for the chemoselective α-nitrosation of β-diketones under mild conditions

A combination of silica sulfuric acid and sodium nitrite in the presence of wet SiO2 was used as an effective nitrosating agent for the nitrosation of β-diketones to their corresponding α-nitroso or α-oximinoketones under mild and heterogenous conditions in moderate to excellent yields.