62050-98-0

Upstream product

• 1008-76-0 4,5-dihydro-5-phenyl-2(3H)-furanone 
• 100-46-9 benzylamine 
• 170805-75-1 N-benzyl-4-hydroxy-4-phenyl-2-butynamide 
• 100-52-7 benzaldehyde 
• 7510-08-9 N-benzyl-4-oxo-4-phenylbutanamide 
• 2051-95-8 succinylbenzene 
• 87605-11-6 propynoic acid benzylamide 

Downstream Products

• 215391-92-7 4-(benzylamino)-1-phenylbutan-1-ol 
• 7510-08-9 N-benzyl-4-oxo-4-phenylbutanamide 

Relevant academic research and scientific papers

THIOETHER TRIAZOLOPYRIDINE AND TRIAZOLOPYRMIDINE INHIBITORS OF MYELOPEROXIDASE

The present invention provides compounds of Formula (I):wherein A, X and Y are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

Palladium-catalyzed selective hydrogenolysis of N-alkyl(aryl)-substituted γ-keto amides as an approach to γ-lactams or linear amides

A palladium-catalyzed hydrogenolysis of N-substituted γ-keto amides can proceed with participation of tautomeric 5-hydroxypyrrolidin-2-ones and give either pyrrolidin-2-ones, or linear amides, or their mixtures, depending on the substrate structure.

Acid promoted cyclodehydration of amino alcohols with amide acetal

A convenient acid-promoted cyclization protocol for the formation of azaheterocycles from amino alcohols is described. The reaction involves the use of N,N-dimethylacetamide dimethyl acetal (DMADA) as the activating reagent of the hydroxyl group. Using this protocol, pyrrolidines or piperidines with various substituents can be synthesized in good to high yields.

Elevation of HDL cholesterol by 4-[(Aminothioxomethyl)-hydrazono]-N-(substituted)-4-arylbutanamides

Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis. These compounds are represented by the formula wherein: R1, R2, and R3are independently hydrogen, C1-C6alkyl, phenyl or —(CH2)1-6phenyl where phenyl is optionally substituted by halogen, cyano, nitro, C1-C6alkyl, C1-C6alkoxy, trifluoromethyl, C1-C6alkoxycarbonyl, —CO2H or OH; R4and R5are independently hydrogen, C1-C10alkyl, C3-C8cycloalkyl, —(CH2)0-6Ar1where Ar1is phenyl, naphthyl, furanyl, pyridinyl or thenyl and Ar1can be optionally substituted by halogen, cyano, nitro, C1-C6alkyl, phenyl, C1-C6alkoxy, phenoxy, trifluoromethyl, C1-C6alkoxycarbonyl, —CO2H or OH, or R4and R5together with the nitrogen to which R4and R5are attached form a ring containing 4-7 carbon atoms; and Ar is phenyl, naphthyl, furanyl, pyridinyl or thienyl which may be optionally substituted by halogen, cyano, nitro, C1-C6alkyl, C3-C6cycloalkyl, phenyl, C1-C6alkoxy, phenoxy, trifluoromethyl, C1-C6alkoxycarbonyl, —CO2H or OH.

Acetylenic Amides. 2. The Generation and Reactions of Dianions Derived From 2-Propynamides

The dianion of N-benzyl-2-propynamide can be generated by the treatment of 4 with two equivalents of LDA at -65 deg C or ethylmagnesium bromide at -20 deg C.The trilithio species 6 is readily formed using 3 equivalents of LDA.Reaction of 5 with aldehydes or ketones produce hydroxypropynamides 9 in good yields.Silation of 5a with chlorotrimethylsilane produces N-benzyl-3-trimethylsilyl-2-propynamide (13) in high yield.Reduction of 9 furnishes either fully saturated amides 15 or partially reduced cis-olefins 16 or 18.Compounds 16, on heating, rearrange to 4-ketoamides 17.Carboxylation of 5a with carbon dioxide produces 3-benzyl-2,4-dioxo-5-oxazidinylacetic acid (11).Warming 11 in dimethyl sulfoxide results in the loss of carbon dioxide and the formation of N-benzylpyruvamide (21).