Quantum-chemistry calculations are performed to study the electronic structures, absorption, phosphorescent, and electroluminescent properties of three color tunable Ir(III) complexes with benzylsulfonyl substituents. The calculated results reveal that substituents para to the metal have a large...
1-Benzylsulfonyl-1,1-dihydropolyfluoroalkan-2-ones react with phthalimidosulfenyl chloride or succinimidosulfenyl chloride to form the sulfenylated products on the active methylene group, 1-benzylsulfonyl-1-phthalimido(succinimido)thiopolyfluoroalkan-2-ones. Decomposition of the latter leads to ...
Activating mutations in the BRAF serine/threonine kinase are found in more than 70% of human melanomas, >90% of which are BRAFV600E. It provides new therapeutic opportunities in malignant melanoma. In silico and in vitro screening of our compound collection has identified Hit 2 as BRAFV600E inhi...
A two-step sequence is reported giving access to diverse 5H-pyrido[2′,1′:2,3]imidazo[4,5-b]indoles and analogues via a Bienaymé multicomponent reaction followed by N-arylation. The desired polycylic scaffolds were obtained in high yield using copper iodide in association with TMEDA in aqueous...
Microbial production of (2S,3S)-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one [(2S,3S)-DHMB], a key intermediate in the synthesis of diltiazem hydrochloride, was investigated. In the course of the screening of microorganisms for the hydrolysis of 3-acetoxy-2-(4-methoxyph...
Leishmaniasis is a group of diseases caused by protozoan parasites from the genus Leishmania. There are estimated 1.3 million new cases annually with a mortality of 20,000–30,000 per year, when patients are left untreated. Current chemotherapeutic drugs available present high toxicity and low e...
A series of 3-(2-(2-methoxyphenyl)-2-oxoethyl) quinazolinone derivatives were designed and synthesized as anticoccidial agents by modifying the quinazoline ring of febrifugine. All the compounds were biologically evaluated according to the ACI method, and four of them exhibited anticoccidial act...
A new class of functionalized 3-(benzofuran-2-yl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole scaffolds (4a–q) was synthesized by a four step reaction in good yields. Initially, o-alkyl derivative of salicyaldehyde (1) readily furnished corresponding 2-acetyl benzofuran (2) on treatment with po...
N-Formyl peptide receptors (FPRs) are G protein-coupled receptors (GPCRs) that play critical roles in inflammatory reactions, and FPR-specific interactions can possibly be used to facilitate the resolution of pathological inflammatory reactions. We here report the synthesis and biological evalua...
Reaction of Mo(CO)6 with excess N,N′-di(3-methoxyphenyl)formamidine (HDmAniF) in o-dichlorobenzene afforded the yellow complex Mo2(DmAniF)4, 1. The structure of 1 reveals that the ligands bridge the two metal centers through the two nitrogen atoms, forming two s-cis, s-trans and two s-trans, s-...
Superacid catalyzed electrophilic substitution of arenes using 4,4,4,-trifluoro/3-trifluoromethylcrotonic acids has been investigated. The direct synthesis of various trifluoromethylated dihydrochalcones, aryl vinyl ketones and indanones has been achieved by this methodology. It has been found t...
Leifsonia xyli HS0904 can stereoselectively catalyze the bioreduction of 3,5-bis(trifluoromethyl) acetophenone (BTAP) to its corresponding alcohol, which is a valuable chiral intermediate in the pharmaceuticals. In this study, a new carbonyl reductase derived from L. xyli HS0904 was purified and...
This paper describes the improved synthesis of n.c.a. 4- 18F]fluorophenol for the preparation of 18F-labeled alkylarylethers. Nucleophilic fluorination of substituted benzophenone derivatives yielded n.c.a. 4- 18F]fluoro-4′-substituted benzophenones with 80– 90 % RCY, which were converted to b...
Trifluoromethyl ketones (TFMKs) significantly contribute to biologically active compounds and special materials. TFMKs can be prepared by “trifluoroacetic ester/ketone metathesis” along with the accompanying products, aromatic acid esters. As an important extension of our previous studies on t...
We synthesized an optically active 4,4,4-trifluoro-3-{4-(4-methoxyphenyl)phenyl}butanoic acid (5*). New chiral dopants for nematic liquid crystals were derived from (R)-(−)-5*, and their helical twisting power (HTP) values were measured. Their HTP values were largely influenced by the linkage be...
Papain from Carica papaya demonstrated catalytic promiscuity was first discovered to catalyze the synthesis of trifluoromethyl carbinol derivatives via aldol reaction between α,α,α-trifluoromethyl ketones and aliphatic ketones in a mixed solvent of DMF and water. The best results of the corre...
Strain D4 was isolated from the sludge of the wastewater treating system of a 4-Chloronitrobenzene (4-CNB) manufacturer. It was able to utilize 4-CNB as the sole carbon and nitrogen source for growth. Strain D4 was preliminarily identified as Cupriavidus sp. based on its physiological & biochemi...
Enzyme-catalyzed enantiomer discrimination is still a great challenge for the development of industrial pharmaceutical processes. For the resolution of ibuprofen, naproxen and ketoprofen racemates, three major anti-inflammatory drugs, only lipases from Candida rugosa present a high selectivity i...
Increased rate of use of fossil fuels have greatly polluted the earth through harmful by-products. Biodiesel is an attractive substitute to fossil fuel in compression ignition engine applications. In this research work, vegetable oil namely Arachis Hypogaea Oil (AHO) is used along with ethanol f...
Biodiesel is a renewable fuel that is commonly used in diesel engines around the world mostly in blends with the conventional diesel. There are many studies concerning its production and its properties and a series of them confirms the biodiesel advantages when compared with conventional diesel ...
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