A mild and general strategy for the synthesis of 2-substituted 4-amino-1,2,4,5-tetrahydro-2-benzazepine-3-ones is described. The seven-membered lactam is prepared by intramolecular amide bond formation from the intermediate amino acid, which is obtained either by reductive alkylation of a variet...

Several new 4-substituted glutamic acid derivatives are described: 4-phosphinomethyl glutamic acid derivatives were prepared starting from (2S)-N-Boc-tert-butyl-4-methylene glutamate. The 4-carboxymethyl and 4-aminomethyl glutamic acid derivatives were obtained using asymmetric 1,4-addition conj...

Glycogen phosphorylase (GP) appears as a key enzyme for the control of hyperglycemia in the context of type 2 diabetes. In order to gain additional data for structure–activity studies of the inhibition of this enzyme, a series of eight GP inhibitor candidates were prepared from peracetylglucopy...

Pure pentanal is irradiated with a frequency tripled Nd-YAG laser in the intensity interval 0.1-1 MW. cm−2. Alpha-dione and α-ketol are formed selectively with quantum yields of 5.5 and 38%, respectively. As only the S1 state of the pentanal is excited, the results obtained are explicable as a ...

Lipid oxidation can adversely alter sensory and nutritional attributes of fats preserved in food powders. The aim of this study was to compare the extent of lipid oxidation in spray dried conventional emulsions and nanoemulsions. Powders containing lactose or lactose/sucrose (7:3) (57.9 g/100 g)...

Dodecamolydbophosphoric acid (HPMo) immobilized on USY zeolite was used as a catalyst for the acetalization of glycerol with pentanal at 70 °C. Catalysts were prepared with different amounts of heteropolyacid, and the most active sample was the [email protected] catalyst (1.1 wt.%). The product...

α-glucosidase inhibition is a rational approach in the effective management of type 2 diabetes. Several inhibitors of this enzyme class are in clinical use, but are riddled with efficacy, potency and safety challenges. For this reason, new effective α-glucosidase inhibitors are under investiga...

GR89696, racemic methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl) methyl]-1-piperazinecarboxylate, a kappa opioid receptor ligand, was labeled with [11C]methyl chloroformate. The radiochemical yield was 20% with an observed specific radioactivity of 75.5 GBq/μmol at end of synthesis (2...

In the present study, we explore Dynamic Mechanical Thermal Analysis (DMTA) as a tool for assessing the physical performance in 19th century paints and to evaluate the parameters that influence the mechanical properties of the paint films. This data is particularly important for accurate life-ti...

The title compound, (E)-1-(3-bromobenzylidene)semicarbazide (3BSC) was synthesized and characterized by FT-IR, FT-Raman, UV, 1HNMR and 13CNMR spectral analysis. The optimized molecular geometry, the vibrational wavenumbers, the infrared intensities and the Raman scattering activities were calcul...

A simple route for the synthesis of 1,4-benzoxazin-3-(4H)-ones is described herein. This method involves the reductive cyclization of 2-(2-nitrophenoxy)acetonitrile adducts in the presence of Fe/acetic acid in good to excellent yields. This system was compatible with various other functional groups.

Neoplastic metastasis is a major process where tumor cells migrate from the primary tumor and colonize at other parts of our body to form secondary tumor. Cancer incidences are rising and novel anti-neoplastic compounds with new mechanism of actions are essential for preventing cancer related de...

SNAr reaction between N-(4,5-dichloro-2-nitrophenyl)acetamide and 4-hydroxybenzoic acid gives 4-(5-acetylamino-2-chloro-4-nitro- phenoxy)benzoic acid and 4-{5-[(5-acetylamino-2-chloro-4-nitrophenyl)amino]-2-chloro-4-nitrophenoxy}benzoic acid which were used for the synthesis of new AB-type monom...

An organocatalytic enantioselective N-nitroso-aldol reaction of 2-oxindoles promoted by a cinchona alkaloid catalyst has been developed. The reaction shows exclusively N-selectivity, affording corresponding products with good to excellent yields (up to 100%) and moderate enantioselectivity. The ...

Replacing one of the morpholine groups of the phosphatidylinositol 3-kinase (PI3K) inhibitor ZSTK474 with a variety of sulfonamide-linked solubilizing substituents produced a new class of active and potent PI3Kα inhibitors, with several derivatives demonstrating high PI3Kα enzyme potency and g...

A unique photoreaction of methyl 6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxylate in methanol gives four β -lactam compounds, methyl 6-chloro-2,9-dioxo-1-methyl-1-azaspiro[3.5]nona-5,7-diene-8-carboxylate and three stereoisomers of dimethyl 3-chloro-4-(1′-methyl-2′-oxoazet...

A facile method has been developed for the preparation of densely functionalized tricyclic fused pyrimidine derivatives by three-component [3+2+1] cyclization. Fairly good yields of the products (up to 88%), the ready availability of the low-cost starting materials, the catalyst-free and mild co...

The transition metal-free intramolecular regioselective domino cyclization of N-Boc protected ynamides has been developed to provide the corresponding tetrahydroisoquinoline-oxazo-2(3H)-ones in moderate to good yields.

Synthetic routes to six 3-D scaffolds containing piperazine, pyrrolidine and piperidine cores have been developed. The synthetic methodology focused on the use of N-Boc α-lithiation-trapping chemistry. Notably, suitably protected and/or functionalised medicinal chemistry building blocks were sy...

We achieved synthesis of seven stereoisomers of 1-C-n-butyl-L-iminofuranose derivatives using catalytic asymmetric alkylation and Negishi coupling as key reactions. The synthetic strategy based on these key reactions was quite useful, since both α- and β-iminofuranoses could be obtained by swi...