85277-78-7

Upstream product

• 16537-09-0 t-butyl phenylacetate 
• 85278-32-6 ethyl 2-phenyl-3,3-difluoroacrylate 
• 22065-57-2 ethyl 2-phenyldiazoacetate 
• 17097-90-4 2-phenylmalonic acid monoethyl ester 
• 101-97-3 Ethyl 2-phenylethanoate 
• 85277-62-9 ethyl 2-(tert-butoxycarbonyl)phenylacetate 

Relevant academic research and scientific papers

Stereoselective Palladium-Catalyzed C?F Bond Alkynylation of Tetrasubstituted gem-Difluoroalkenes

A stereoselective Pd(PPh3)4-catalyzed C?F bond alkynylation of tetrasubstituted gem-difluoroalkenes with terminal alkynes has been developed. This method gives access to a great variety of conjugated monofluoroenynes bearing a tetrasubstituted alkene moiety with well-defined stereochemistry. Chelation-assisted oxidative addition of Pd to the C?F bond is proposed to account for the high level of stereocontrol. An X-ray crystal structure of a key monofluorovinyl PdII intermediate has been obtained for the first time as evidence for the proposed mechanism.

Nucleophilic Vinylic Substitution (SNV) of Trisubstituted Monofluoroalkenes for the Synthesis of Stereodefined Trisubstituted Alkenes and Divinyl Ethers

We herein describe a nucleophilic vinylic substitution (SNV) of trisubstituted monofluoroalkenes with excellent stereocontrol (d.r. > 99:1). Starting from (E)-β-monofluoroacrylates, various trisubstituted (E)-alkenes containing O/N/S-substituent groups at the vinylic position can be obtained under simple conditions. Furthermore, (E,E)-divinyl ethers can be generated through dimerization of the monofluoroalkenes, triggered by adventitious water in the reaction mixture.

Palladium-Catalyzed Stereoselective Hydrodefluorination of Tetrasubstituted gem-Difluoroalkenes

A highly stereoselective palladium(0)-catalyzed hydrodefluorination (HDF) of tetrasubstituted gem-difluoroalkenes is developed. By using catalytic Pd(PPh3)4 (2.5-5 mol percent) and hydrosilane Me2PhSiH, various trisubstituted terminal (E)-monofluoroalkenes can be synthesized with excellent E/Z selectivity (>99:1) and good functional group tolerability. The key stereocontrol should be exerted by an ester-directed C-F bond oxidative addition step in the catalytic cycle.

Novel arylalkenylpropargylamines as neuroprotective, potent, and selective monoamine oxidase B inhibitors for the treatment of Parkinson's disease

To develop novel neuroprotective agents, a library of novel arylalkenylpropargylamines was synthesized and tested for inhibitory activities against monoamine oxidases. From this, a number of highly potent and selective monoamine oxidase B inhibitors were identified. Selected compounds were also tested for neuroprotection in in vitro studies with PC-12 cells treated with 6-OHDA and rotenone, respectively. It was observed that some of the compounds tested yielded a marked increase in survival in PC-12 cells treated with the neurotoxins. This indicates that these propargylamines are able to confer protection against the effects of the toxins and may also be considered as novel disease-modifying anti-Parkinsonian agents, which are much needed for the therapy of Parkinson's disease.

Enzyme-activated irreversible inhibitors of monoamine oxidase: Phenylallylamine structure-activity relationships

Seventeen 2-aryl-3-haloallylamine derivatives were prepared and evaluated as inhibitors of monoamine oxidase (MAO, EC 1.4.3.4). The synthesis of these compounds was achieved from either α-methylstyrene or ring-substituted phenylacetic acid derivatives. Wi

Allyl amine MAO inhibitors

Compounds of the formula STR1 wherein: R is phenyl, phenyl monosubstituted, disubstituted, or trisubstituted by (C1 -C8) alkyl, (C1 -C8)alkoxy, hydroxy, chlorine, bromine, iodine, fluorine, trifluoromethyl, nitr