Convenient and Scalable Synthesis of 2,3-Dihydroquinazolin-4(1H)-one Derivatives and Their Anticancer Activities

An efficient and mild InBr₃-catalyzed approach to synthesize 2,3-dihydroquinazolin-4(1H)-one derivatives (3a–3aa) has been developed. Notably, all the products were isolated by recrystallization and the reaction is accessible on a gram scale. Moreover, the reactions only require 10–60 min. All the synthesized compounds were evaluated for their in vitro anticancer activity against four human cancer cell lines.     

Efficient and Industrially Viable Synthesis of Donepezil

An efficient, economically viable process has been developed for large‐scale preparation of donepezil HCl (1), an anti‐Alzheimer's agent. The process involves the condensation of 5,6‐dimethoxy‐1‐indanone (3) and 1‐benzyl‐4‐piperidinecarboxaldehyde (4) in the presence of alkalimetal carbonates at elevated temperature to yield 1‐benzyl‐4‐[(5,6‐dimethoxy‐1‐indanone)‐2‐yidenyl] methyl piperidine (2), the key intermediate in the synthesis of donepezil. Hydrogenation of 2 yields donepezil.     

Regiospecific Preparation of 5-Acylaminotetralones

A Beckmann Rearrangement/Friedel-Crafts strategy was utilized to prepare 5-amidotetralones in high yield.     

PCC-Promoted Dehydration of Aldoximes: A Convenient Access to Aromatic,Heteroaromatic, and Aliphatic Nitriles

A simple and convenient procedure for the synthesis of nitriles by dehydration of aldoximes using a PCC (pyridiniumchlorochromate) has been developed. A variety of aromatic, heteroaromatic, and aliphatic aldoximes are converted.

Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the full spectral details.     

Synthesis of gemini surfactants with twelve symmetric fluorine atoms and one singlet F MR signal as novel F MRI agents

A family of fluorinated gemini surfactants derived from perfluoropinacol has been synthesized as novel ¹⁹F magnetic resonance imaging (¹⁹F MRI) agents. These fluorinated surfactants with 12 symmetric fluorine atoms and one singlet ¹⁹F MR peak can be conveniently prepared from perfluoropinacol and oligo(ethylene glycols) on multi-gram scales. Solubility, hydrophilicity (log P), and critical micelle concentration (CMC) measurements of these fluorinated surfactants indicated that high aqueous solubility can be achieved by introducing oligo(ethylene glycols) with appropriate length into perfluoropinacol, i.e., manipulating the fluorine content (F%). One of these fluorinated surfactants with high aqueous solubility and excellent ¹⁹F MR properties has been identified by ¹⁹F MRI phantom experiments as a promising ¹⁹F MRI agent.     

Poly(ethylene terephthalate) waste derived chemicals as an antistripping additive for bitumen – An environment friendly approach for disposal of environmentally hazardous material

The increasing accumulation of poly(ethylene terephthalate) polymer and poor recycle/disposal practices have made them omnipresent and a major culprit for environmental pollution. Currently global research efforts are focused on primary and secondary recycling of PET waste or through landfills. Chemical recycling of PET through hydrolytic or aminolytic route has been attempted by many researchers however with limited end applications. In our investigations we have used PET waste as a synthon and chemically converted it through a new non-catalytic route into several benzamide derivatives. We have successfully tested them for antistripping performance in bitumen. Our results as elaborated in the paper indicate a comparable performance of the new chemistry products based on PET, to commercially used antistripping chemicals. Our research work thus opens a new route for the recycling of used PET in bituminous concrete roads which may help in alleviating a major environmental problem and disposal of waste PET polymer in large scale.     

The Hydrotrope Action of Vitamin C

The effects of vitamin C are determined in the oil-in-water(0/ W) and water-in-oil(W/ 0) microemulsion regions of CTAB/ pentanol/ p-xylene/ H20 system. The addition of Vc joins the O/ W and W/ O areas in the phase diagram and expands the bicontinous region by reducing the lamellar liquid crystal one. The results show that the “ coupling action” of Vc is in fact a structural transition from lamellar crystal to isotropic phase with W/ O, O/ W and bicontinous structure.     

An enantioselective synthesis of a MEM-protected aetheramide A derivative

Aetheramides A and B are very potent anti-HIV agents. An enantioselective synthesis of a MEM-protected aetheramide A derivative is described. The synthesis was accomplished in a convergent and stereoselective manner. The key reactions involved asymmetric dihydroxylation, asymmetric allylation, asymmetric syn-aldol reactions, and asymmetric hydrogenation.     

Gram-scale synthesis of anti-pancreatic flavonoids (±)-8-[1-(4′-hydroxy-3′-methoxyphenyl)prop-2-en-1-yl]-chrysin and -galangin

Gram-scale total synthesis of (±)-8-[1-(4′-hydroxy-3′-methoxyphenyl)prop-2-en-1-yl]-galangin (1) and -chrysin (2) has been accomplished in eight steps from commercially available phloroglucinol and three steps from commercially available chrysin, respectively, featuring an efficient introduction of C(8) (1-prop-2-en-1-yl)phenyl moiety in the natural products through chemo- and regioselective cinnamylation and regioselective aromatic Claisen rearrangement.     

以四甲基铵硅酸盐为柱化剂合成层柱状MCM-36分子筛

以层状MCM-22P为前驱体,四甲基铵硅酸盐为柱化剂,采用动态水热法考察了MCM-36分子筛的合成条件,并通过XRD、N2物理吸附、TEM、27Al-MAS NMR以及NH3-TPD等手段对合成分子筛进行了表征。结果表明,与传统的采用正硅酸乙酯为柱化剂的柱化过程相比,以四甲基铵硅酸盐为柱化剂时,已溶胀的前驱体不经干燥处理即可直接在含水体系进行柱化插层合成得到层间距均一的层柱状MCM-36分子筛,适宜的合成条件为:先在80℃的高pH值(约13.5)环境下对前驱体溶胀24 h,然后在100℃下柱化插层24 h。表征结果表明,MCM-36分子筛具有层内微孔和层间介孔的复合孔道结构以及较大的比表面积(特别是外比表面积);与HMCM-22相比,HMCM-36的表面酸性虽明显降低,但其层间介孔结构的形成使大量B酸中心暴露于大分子易于接近的层间介孔孔壁,可为涉及较大分子的催化反应提供更多可接近的活性位中心。