29943-30-4

Upstream product

• 17431-94-6 2-phenylsulfanyl-propionic acid 
• 108-98-5 thiophenol 
• 108-86-1 bromobenzene 

Downstream Products

• 59792-92-6 1-Pentyl-2-propenyl 2-(phenylthio)propanol 
• 129959-68-8 1-tert-Butyl-3-methyl-3-phenylsulfanyl-4-((E)-styryl)-azetidin-2-one 
• 135616-62-5 (3S,4S)-4-Benzoyl-1-(4-methoxy-phenyl)-3-methyl-3-phenylsulfanyl-azetidin-2-one 
• 135616-62-5 (3S,4R)-4-Benzoyl-1-(4-methoxy-phenyl)-3-methyl-3-phenylsulfanyl-azetidin-2-one 
• 135616-48-7 (3S,4S)-1-(4-Methoxy-phenyl)-3-methyl-3-phenylsulfanyl-4-((E)-styryl)-azetidin-2-one 
• 135616-48-7 (3S,4R)-1-(4-Methoxy-phenyl)-3-methyl-3-phenylsulfanyl-4-((E)-styryl)-azetidin-2-one 
• 135616-64-7 (2S,3S)-1-(4-Methoxy-phenyl)-3-methyl-4-oxo-3-phenylsulfanyl-azetidine-2-carboxylic acid methyl ester 
• 135616-64-7 (2R,3S)-1-(4-Methoxy-phenyl)-3-methyl-4-oxo-3-phenylsulfanyl-azetidine-2-carboxylic acid methyl ester 
• 77161-76-3 2,4-bis(phenylthio)-3-pentanone 
• 135616-66-9 (3S,4S)-1-(4-Methoxy-phenyl)-3-methyl-4-phenylethynyl-3-phenylsulfanyl-azetidin-2-one 
• 135616-66-9 (3S,4R)-1-(4-Methoxy-phenyl)-3-methyl-4-phenylethynyl-3-phenylsulfanyl-azetidin-2-one 
• 127055-15-6 (3S,4R)-4-((E)-1,2-Diphenyl-vinyl)-1-(4-methoxy-phenyl)-3-methyl-3-phenylsulfanyl-azetidin-2-one 
• 135616-57-8 (3S,4S)-1-(4-Methoxy-phenyl)-3-methyl-4,5-diphenyl-3,4-dihydro-1H-pyridin-2-one 
• 135616-51-2 (S)-1-(4-Methoxy-phenyl)-3-methyl-4,5-diphenyl-3-phenylsulfanyl-3,4-dihydro-1H-pyridin-2-one 

Relevant academic research and scientific papers

Complete assignment of 1H and 13C NMR spectra of some α-arylthio and α-arylsulfonyl substituted N-methoxy-N-methyl propionamides

The complete assignments of the 1H and 13C NMR spectra of the some α-arylthio and α-arylsulfonyl substituted N-methoxy-N-methyl propionamides, bearing methoxy, methyl, chloro, and nitro as substituents at the phenyl ring are reported

Trichosporon beigelli esterase (TBE): A versatile esterase for the resolution of economically important racemates

A hydrolase producing strain Trichosporon beigelli esterase (TBE) isolated from local cottage cheese in its native form has displayed versatility and high efficacy in the kinetic resolution of a wide range of economically important substrates, which include racemic secondary alcohols, such as 1-(6-methoxy-2-naphthyl)ethanol (E ～ 316), 1-(3,4-methylenedioxyphenyl) ethanol and pentanol (E ～ 180 and 156 resp.), and alkyl esters of carboxylic acids such as ibuprofen (E ～ 340), 2-(benzylthio)propanoic acid (E ～ 1000). In other substrates such as in the primary alcohol 2-(6-methoxy-2- naphthyl)propan-1-ol and carboxylic acids such as 2-(5-bromo-6-methoxy-2- naphthyl)propanoic acid, 2-(2-naphthyloxy)propanoic acid, and substituted 2-thiopropanoic acids, it displayed moderate to low selectivity. Commercial lipases such as CCL, PPL, and PSL were also used in the resolution of the substrates for comparative studies.

Oligomeric aminodiol-containing compounds, libraries thereof, and process of preparing the same

Oligomeric compounds comprising a plurality of aminodiol monomer subunits joined by linking groups are provided, as well as libraries of such compounds and processes for preparing the oligomeric compounds and libraries.

Amine compounds and combinatorial libraries comprising same

The present invention provides monocyclic, bicyclic and oligomeric amine compounds with at least two sites of diversity. These compounds are formed from monocyclic scaffolds which can be cyclized to form bicyclic amine scaffolds. These can then be reacted with building blocks to form the amine compounds of the invention. This invention further provides libraries or monocyclic, bicyclic and oligomeric amine compounds. Also provided are methods for preparing monocyclic, bicyclic and oligomeric amine compounds and libraries thereof. The present invention also provides pharmaceutical compositions of the monocyclic, bicyclic and oligomeric amine compounds.

2-(4-R-Phenoxy/phenylthio)alkanoic esters of l-lupinine

Considering the great pharmacological interest in phenoxy/phenylthioalkanoic esters of open-chain or cyclic aminoalcohols, a set of ten such esters of lupinine was prepared. Initially, their ability to displace [3H]QNB from rat brain preparation was investigated. With the exception of two, all the prepared esters exhibited good affinity to muscarinic receptors (on a non-selective basis), with pKi in the range 6.67-7.68.

Dynamic enzymatic resolution of thioesters

A detailed investigation of several issues related to the enzymatic resolution of thioesters under conditions of continuous racemization of substrate was conducted. The kinetic acidity of the α-protons of a series of α-substituted propionate thioesters was studied. It was found that the rate of α-proton exchange could be enhanced as much as 20-fold by variation of the thiol moiety, increasing the range of compounds to which enzymatic dynamic resolution may be applied. The relative rates of hydrolysis of ethyl butyrate and ethyl thiobutyrate by several enzymes commonly used in enzymatic resolution were determined. All of the enzymes studied exhibited similar rates of thioester and oxoester hydrolysis except for the esterase from pig liver, which showed very low activity in thioester hydrolysis. Dynamic resolution of the propargyl and trifluoroethyl thioesters of α- phenylpropionate was conducted using subtilisin Carlsberg as a catalyst. These examples demonstrated that enzymatic dynamic resolution can be applied even when the rate of α-proton exchange and the enantioselectivity of the enzyme are fairly low. A dynamic enzymatic transesterification procedure was demonstrated in the resolution of the trifluoroethyl thioester of α-(2,4- dichlorophenoxy)propionate, and product was obtained in 93% ee. This work helps expand and define the scope of enzymatic dynamic resolution of thioesters.

Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 2. 2-Phenoxy-, 2-(phenylthio)-, and 2-(phenylamino)alkanoic acid esters

Further modifications of the leads ((R)-(+)-hyoscyamine and (p- chlorophenyl)propionic acid α-tropanyl ester), which show analgesic and nootropic activities as a consequence of increased central presynaptic ACh release, are reported. 2-Phenoxy- and 2-(phenylthio)alkanoic acid esters showed the best results. Several members of these classes possess analgesic properties which are comparable to that of morphine and at the same time are able to reverse dicyclomine-induced amnesia. Confirmation was found that the mechanism of action is due to an increase in ACh release at central muscarinic synapses and that both auto- and heteroreceptors controlling ACh release are very likely involved. According to the results obtained with (R)- (+)-hyoscyamine, analgesic activity is stereochemistry dependent, since the R-(+)-enantiomers are always more efficacious than the corresponding S-(-)- ones. On the basis of their potency and acute toxicity, compounds (±)-28 (SM21) and (±)-42 (SM32) were selected for further study.