17946-01-9

Upstream product

• 3395-91-3 Methyl 3-bromopropionate 
• 103-67-3 benzyl-methyl-amine 
• 292638-85-8 acrylic acid methyl ester 

Downstream Products

• 24549-12-0 methyl 3-(methylamino)propanoate 
• 2213-08-3 ethyl 3-methylaminopropionate 
• 149692-49-9 3-(N-Benzyl-N-methylamino)propionsaeure 
• 124078-87-1 3-(4-phenyl-1-piperazinyl)-propionic acid 
• 65845-56-9 3-(methylamino)propanoic acid hydrochloride 
• 5814-42-6 3-(N-benzyl-N-methylamino)-propan-1-ol 
• 98217-46-0 N-<2-(methoxycarbonyl)ethyl>-N-methyl-3-phenylpropynamide 
• 17946-02-0 4-(benzylmethylamino)-2-methylbutan-2-ol 

Relevant academic research and scientific papers

Synthesis of 64CuII- bis(dithiocarbamatebisphosphonate) and its conjugation with superparamagnetic iron oxide nanoparticles: In vivo evaluation as dual-modality PET-MRI agent

A novel bifunctional chelator combines a dithiocarbamate group for binding the positron-emitter 64Cu (red spheres) for PET imaging and a bisphosphonate group (green ellipsoids) for strong binding to several inorganic materials, such as MRI cont

Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease

In this study, four series of compounds with benzoxazolone and benzothiazolone cores were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease (AD). Additionally, in order to shed light on the effect of the carbonyl groups of benzoxazolone/benzothiazolone, benzoxazole/benzothiazole-containing analogues were also synthesized and evaluated. Inhibition potency of all final compounds towards cholinesterase enzymes and their antioxidant activity were tested. Subsequently, the anti-inflammatory activity, cytotoxicity, apoptosis, and Aβ aggregation inhibition tests were also performed for selected compounds. The results indicated that compounds 11c, a pentanamide derivative with benzothiazolone core, and 14b, a keton derivative with benzothiazolone core, were considered as promising multi-functional agents for further investigation against AD. The reversibility, kinetic and molecular docking studies were also performed for the compounds with the highest AChE 14b (eeAChE IC50 = 0.34 μM, huAChE IC50 = 0.46 μM) and BChE 11c (eqBChE IC50 = 2.98 μM, huBChE IC50 = 2.56 μM) inhibitory activities.

SULFOXIDE-BASED REAGENT FOR MASS SPECTROMETRY

The present invention relates to sulfoxide-based reagents suitable in the mass spectrometric determination of analyte molecules such as peptides as well as adducts of such reagents and analyte molecules and applications of said reagents and adducts. Further, the present invention relates to methods for the mass spectrometric determination of analyte molecules.

A Sulfoxide-Based Isobaric Labelling Reagent for Accurate Quantitative Mass Spectrometry

Modern proteomics requires reagents for exact quantification of peptides in complex mixtures. Peptide labelling is most typically achieved with isobaric tags that consist of a balancer and a reporter part that separate in the gas phase. An ingenious distribution of stable isotopes provides multiple reagents with identical molecular weight but a different mass of the reporter groups, allowing relative quantification of multiple samples in one measurement. Here we report a new isobaric labelling reagent, where the balancer and the reporter are linked by a sulfoxide group, which, based on the sulfoxide pyrolysis, leads to easy and asymmetric cleavage at low fragmentation energy. The fragmentation of our new design is significantly improved, yielding more intense complementary ion signals, allowing complementary ion cluster analysis as well.

Lipase immobilization on hyroxypropyl methyl cellulose support and its applications for chemo-selective synthesis of β-amino ester compounds

The present study carried out the synthesis of β-amino ester compounds using lipase immobilized on hyroxypropyl methyl cellulose (HMC) support. Initially various lipases (biocatalysts) from different origin were immobilized and subsequently screened to obtain the robust biocatalyst. The lipase Pseudomonas fluorescence (PFL) immobilized on HMC was displayed highest lipase activity, protein content and retention of activity. The physical and biochemical characterization verified immobilization of lipase PFL on the HMC support. This immobilized biocatalyst HMC:PFL (3.5:1) was successfully applied for the practical biocatalytic applications to synthesize variety of β-amino esters. Various eight reaction parameters were optimized in details to achieve the maximum yield and chemo-selectively. The developed biocatalytic protocol was successfully applied to synthesize different industrially important β-amino esters compounds (21 substrates) with an excellent yield (>90%) and remarkable chemo selectivity (>94%). Interestingly, the immobilized HMC:PFL lipase showed 2.1–2.5 folds higher bio-catalytic activity and five times recyclability as compared to the free PFL. The plausible mechanism for lipase catalyzed synthesis of β-amino ester compounds was also proposed.

Synthesis of 3-(2-aminoethyl)-5-hydroxy-1H-pyrazole derivatives

Treatment of β-keto ester 8 with hydrazines 9a-g gave 1'-substituted tert-butyl 2-(5-hydroxy-1Hpyrazol- 3-yl)ethylcarbamates 10a-e and 2-(5-oxo-2,5-dihydro-1H-pyrazol-3-yl)ethylcarbamates 11f,g. Acidolytic deprotection of 10b,c afforded the corresponding 3-(2-aminoethyl)-5-hydroxy- 1H-pyrazoles 6b,c in good yields. Acylation of 6 gave either the N-acyl compounds 12b,c and 13c, or the N,O-diacyl derivative 14. Next, three N,N-dialkyl analogues 15a,b and 26c were prepared from dimethyl acetone-1,3-dicarboxylate 21 via condensation with hydrazines 9a and 9h followed by hydrolysis of the esters 22a,b, amidation of the carboxylic acids 23a,b, and reduction of the tertiary carboxamides 24a and 25b,c. ARKAT-USA, Inc.

BISPHOSPHONATE COMPOUNDS FOR CHELATING RADIONUCLIDES

Bisphosphonate compounds for chelating radionuclides are described which have separate bisphosphonate and metal chelating groups joined by a linker, so that the bisphosphonate groups are available to complex to hydroxyapatite in bone, while the metal chelating group binds to the radionuclide. This avoids problems in the prior art, where the bisphosphonate groups are used for both binding functions which compromises the bone-seeking activity of the bisphosphonate groups when they are used to chelate the radionuclide.

Silicon tetrachloride catalyzed aza-michael addition of amines to conjugated alkenes under solvent-free conditions

The efficient and very simple conjugate addition of aromatic and aliphatic amines to α,β-unsaturated carbonyl compounds under solvent-free conditions in the presence of catalytic amount of silicon tetrachloride is reported. The reaction of aryl and alkyl amines with different Michael acceptors gave the corresponding Michael adducts with simple catalyst and good to excellent yields. Georg Thieme Verlag Stuttgart New York.

Imidazolium-based polymer supported gadolinium triflate as a heterogeneous recyclable Lewis acid catalyst for Michael additions

A heterogeneous Lewis acid catalytic system has been developed by incorporating gadolinium triflate on to poly[styrene-co-(1-((4-vinylphenyl)methyl)-3-methylimidazolium) tetrafluoroborate] (1-Gd(OTf)3), and the catalytic activity of this system has been examined for Michael additions of amines and thiols to α,β-unsaturated esters and acrylonitrile. The reactions proceed in moderate to excellent yields in the presence of catalytic system 1-Gd(OTf)3. The catalytic system could be efficiently recycled and reused.

1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU)-promoted efficient and versatile aza-Michael addition

A convenient and versatile method was developed for aza-Michael addition using a substoichiometric amount of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU). Various nitrogen nucleophiles were efficiently introduced to α,β-unsaturated carbonyl compounds employing 0.5 equiv of DBU. Furthermore, other heteroatomic nucleophiles could also be introduced successfully under the same reaction conditions.