Getting in there: Efficient intracellular delivery of anticancer drugs is achieved by using reversibly cross-linked dextran nanoparticles, which are rapidly destabilized under reductive environments that mimic those the compartments. These nanoparticles show high drug loading efficiency and reduction-triggered release doxorubicin vitro as well inside tumor cells, particularly to cell nucleus (see scheme). Detailed facts importance specialist readers published "Supporting Information". Such...

An efficient one-pot synthesis of spirooxindole derivatives by three-component reaction isatins, malononitrile (cyanoacetic ester) and 1,3-dicarbonyl compounds in water the presence l-proline is reported. This new protocol has advantages environmental friendliness, higher yields, shorter times, low cost, convenient operation.

The abnormal expression of tumor-related proteases plays a critical role in cancer invasion, progression, and metastasis. Therefore, it is considerably meaningful to non-invasively assess the proteases' activity vivo for both tumor diagnosis therapeutic evaluation. Herein, we report an activatable probe constructed with near-infrared dye (Cy5.5) quencher (QSY21) covalently linked through peptide substrate matrix metalloproteinases-2 (MMP-2) that was chosen as model tumor-associated...

pH-responsive biodegradable micelles were prepared from block copolymers comprising of a novel acid-labile polycarbonate hydrophobe and poly(ethylene glycol) (PEG). Two new cyclic aliphatic carbonate monomers, mono-2,4,6-trimethoxybenzylidene-pentaerythritol (TMBPEC, 2a) mono-4-methoxybenzylidene-pentaerythritol (MBPEC, 2b) designed successfully synthesized via two-step procedure. The ring-opening polymerization 2a or 2b in the presence methoxy PEG dichloromethane at 50 °C using zinc...

An intriguing new Wacker-type oxidation of alkynes catalyzed by PdBr2 and CuBr2 is described, which opens an efficient access to 1,2-diketones using molecular oxygen. Under the optimized conditions, a variety alkynes, including diarylalkynes, arylalkylalkynes, dialkylalkynes, were compatible substrates in this transformation. The mechanism reaction was preliminarily investigated control experiments.

An efficient one-pot synthesis of 4,5,6-triaryl-3,4-dihydropyrimidin-2(1H)-ones via a three-component Biginelli-type condensation aldehyde, 2-phenylacetophenone, and urea/thiourea in the presence catalytic amount t-BuOK (20 mol %) is described. The reactions proceeded efficiently at 70 °C to afford desired products moderate good yields. Detailed mechanistic study shows that reaction using urea thiourea proceeds through two totally different pathways. Enone 5 bis-urea 8 were highly suggested...

Abstract Chalcogen-containing compounds have received considerable attention because of their manifold applications in agrochemicals, pharmaceuticals, and material science. While many classical methods been developed for preparing organic sulfides, most them exploited the transition-metal-catalyzed cross-couplings aryl halides or pseudo with thiols disulfides, harsh reaction conditions usually being required. Herein, we present a user-friendly, nickel-catalyzed reductive thiolation...

By introducing a coplanar fluorenone into the center of an azo molecule, turn-on voltages ternary memory devices are significantly decreased to lower than –2 V due improved crystallinity and reduced charge injection barrier. The resulting low-power consumption will have great potential applications in high-performance chips for future portable nanoelectronic devices. Detailed facts importance specialist readers published as "Supporting Information". Such documents peer-reviewed, but not...

A novel palladium-catalyzed three-component reaction for the synthesis of quinazolin-4(3H)-ones from readily available 2-aminobenzamides and aryl halides via a isocyanide insertion/cyclization sequence has been developed. This methodology efficiently constructs in moderate to excellent yields with advantages operational simplicity.

An efficient I2 (20 mol %)/TBPB mediated oxidative formal [4 + 1] cycloaddition of N-tosylhydrazones with anilines via C–N/N–N bond formation and S–N cleavage has been developed. This protocol represents a simple, general, approach for the construction 1,2,3-triazoles under metal-free azide-free conditions by utilizing catalytic amount I2.

ADVERTISEMENT RETURN TO ISSUEPREVLetterNEXTSynthesis of Isatins by I2/TBHP Mediated Oxidation IndolesYou Zi, Zhong-Jian Cai, Shun-Yi Wang*, and Shun-Jun Ji*View Author Information Key Laboratory Organic Synthesis Jiangsu Province, College Chemistry, Chemical Engineering Materials Science & Collaborative Innovation Center Suzhou Nano Technology, Soochow University, 215123, China*E-mail: [email protected]*E-mail: protected]Cite this: Org. Lett. 2014, 16, 11, 3094–3097Publication Date (Web):May...

A novel radical phosphinylation of α,α-diaryl allylic alcohols with arylphosphine oxides was described for the direct preparation α-aryl-β-phosphinylated carbonyl ketones in medium to good yields via 1,2-aryl migration. In this reaction, formation new C(Ar)–C(sp3) and C(sp3)–P bonds observed.

A novel catalyst-free one-pot tandem reaction for the stereoselective construction of polycyclic spiroindolines was developed. This method offers a straightforward access to structurally diverse spiroindoline derivatives in high yields (up 90%) with excellent levels diastereoselectivity.

An efficient synthesis of polyhydroquinoline derivatives were reported via four-component coupling reactions aldehydes, dimedone, ethyl acetoacetate and ammonium acetate in the presence a catalytic amount ionic liquid under solvent free conditions. In meantime, effect different liquids on reaction has also been investigated.

A novel and highly efficient strategy for the synthesis of isocoumarins phthalides through a palladium(0)-catalyzed reaction incorporating tert-butyl isocyanide has been developed. This process, providing one simplest methods this class valuable lactones, involves two steps including cyclization simple acid hydrolysis. The methodology is tolerant wide range substrates applicable to library synthesis.

A Co(II)-catalyzed synthesis of sulfonyl guanidines by using amines, isonitriles, and organic azides as nitrene sources has been developed. This protocol provides an environmentally friendly simple strategy for the guanidine derivatives employing a range substrates will find potential applications in synthesis. The computational EPR studies suggested formation via cobalt–nitrene radical intermediate.

Abstract Compared with the well‐known palladium‐catalyzed oxidative dehydrogenation coupling reactions, similar transforms initiated by copper/oxygen have attracted more and attention. We investigated a novel construction of heteroaromatic imidazo[1,2‐ ]pyridines through copper(I) iodide/boron trifluoride etherate/oxygen‐mediated dehydrogenative reactions aryl alkyl or ketones 2‐aminopyridines. Four hydrogen atoms are removed two new CN bonds formed in one step via imine formation C( sp 3...

A novel CuI/BF(3)·Et(2)O/O(2)-mediated reaction utilizing ketones and benzylamines for the construction of substituted imidazoles in one step under mild conditions has been demonstrated. This protocol involved removal eight hydrogen atoms, functionalization four C(sp(3))-H bonds three new C-N bond formations.

Cobalt catalysis: Synthesis of substituted 2-aminobenzimidazoles, 2-aminobenzothiazoles, and 2-aminobenzoxazoles was achieved by using cobalt(II) acetate catalyzed isocyanide insertion to o-diaminobenzene, 2-aminobenzenethiol, 2-aminophenol derivatives in 1,4-dioxane (see scheme). It found that the reaction proceeded efficiently give desired products up 95 % isolated yields C-N C-S (O, N) formation a single step.

A nickel-catalyzed defluorinative reductive cross-coupling of gem-difluoroalkenes with thiosulfonate or selenosulfonates is described. The reaction involves the formation thiolated selenylated monofluoroolefins via regioselective C–F bond cleavage and C–S C–Se features easily available substrates, mild conditions, high E-selectivity. One derivatives by further cross coupling PhMgBr exhibited an aggregation-induced emission enhancement effect.

Abstract A metal‐free direct alkylation of simple carbonyl compounds (ketones, esters, and amides) with α,α‐diaryl allylic alcohols is described. The protocol provides facile access to highly functionalized dicarbonyl ketones by a radical addition/1,2‐aryl migration cascade. regioselectivity the reaction was precisely controlled nature compound.