60314-64-9

Upstream product

• 455-14-1 4-trifluoromethylphenylamine 
• 15486-96-1 3-Bromopropionyl chloride 
• 930-21-2 2-azetidinone 
• 402-43-7 p-trifluoromethylphenyl bromide 
• 3798-77-4 3-bromo-N-[4-(trifluoromethyl)phenyl]propanamide 

Relevant academic research and scientific papers

Palladium-catalyzed coupling of lactams with bromobenzenes

An efficient method for the coupling of lactams with bromobenzenes mediated by palladium acetate and DPPF is presented. The reaction proceeds efficiency with a variety of lactams and both electron-rich and poor substituted bromobenzenes.

Enantioselective Synthesis of Cyclopropanone Equivalents and Application to the Formation of Chiral β-Lactams

Cyclopropanone derivatives have long been considered unsustainable synthetic intermediates because of their extreme strain and kinetic instability. Reported here is the enantioselective synthesis of 1-sulfonylcyclopropanols, as stable yet powerful equivalents of the corresponding cyclopropanone derivatives, by α-hydroxylation of sulfonylcyclopropanes using a bis(silyl) peroxide as the electrophilic oxygen source. This work constitutes the first general approach to enantioenriched cyclopropanone derivatives. Both the electronic and steric nature of the sulfonyl moiety, which serves as a base-labile protecting group and confers crystallinity to these cyclopropanone precursors, were found to have a crucial impact on the rate of equilibration to the corresponding cyclopropanone. The utility of these cyclopropanone surrogates is demonstrated in a mild and stereospecific formal [3+1] cycloaddition with simple hydroxylamines, leading to the efficient formation of chiral β-lactam derivatives.

Synthesis of new tricyclic 5,6-dihydro-4H-benzo[b][1,2,4]tri-azolo[1,5-d][1,4]diazepine derivatives by [3+ + 2]-cyclo-addition/rearrangement reactions

Two new series of tricyclic heterocycles, namely 5,6-dihydro-4H-benzo[b][1,2,4]triazolo[1,5-d][1,4]diazepinium salts 10 and the related neutral, free bases 13 were synthesized from 4-acetoxy-1-acetyl-4-phenylazo-1,2,3,4-tetrahydroquinolines 8 and nitriles 9 in the presence of aluminium chloride by the [3+ + 2]-cycloaddition reaction of the in situ generated azocarbenium intermediates 14 followed by a ring-expansion rearrangement. In the rearrangement reaction, the phenyl substituent in the initially formed spiro-triazolium adducts 16 underwent a [1,2]-migration from C(3) to the electron-deficient N(2). This led to the ring expansion from 6-membered piperidine to 7-membered diazepine furnishing the tricyclic 1,2,4-triazole-fused 1,4-benzodiazepines.

Amino-substituted imidazo[1,2-a]pyridinecarboxamides and their use

The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

ANILINE DERIVATIVES

The present invention provides a novel compound having a kininogenase-inhibitory action and its pharmaceutical use. The compounds represented by the formulas (A), (B), (C), (E) and (H) : wherein each symbol is as defined in the specification, or a pharmac

Herbicidal N-aryl substituted azetidinones

Disclosed are herbicidal compositions comprising an inert carrier and as an essential active ingredient in a quantity toxic to weeds a compound of the formula EQU1 wherein X is selected from the group consisting of alkyl, alkenyl, alkoxy, alkylthio, halogen, haloalkyl and nitro; and n is an integer from 0 to 5.