Described herein is the discovery of a novel series antitumor sulfonamides targeting G1 phase cell cycle. Cell cycle control in has attracted considerable attention recent cancer research, because many important proteins involved progression or G1/S transition have been found to play crucial role proliferation, differentiation, transformation, and programmed death (apoptosis). We previously reported our first sulfonamide E7010 as tubulin polymerization inhibitor. Interestingly enough,...

[reaction--see text] Indoles are selectively acylated at the 3-position in high yields on treatment with a wide variety of acyl chlorides CH(2)Cl(2) presence diethylaluminum chloride or dimethylaluminum chloride. The reaction proceeds under mild conditions and is applicable to indoles bearing various functional groups without NH protection.

Abstract Cation radicals of enamines, generated by the oxidation with CeIV compounds, react electron-rich olefins to give addition products. The formal α-alkylation formylacetate is realized reaction 3-(1-pyrrolidinyl)propenoate and use tetrabutylammonium cerium(IV) nitrate as an oxidant.

β,β-Difluorostyrenes bearing tosylamido, hydroxy ormethylsulfinyl groups at the o-position undergo intramol-ecular substitution of nitrogen, oxygen or sulfur withloss fluorine via a 5-endo-trigonal process leading to2-fluorinated heterocyclic systems in high yields.

Abstract Organic azides were prepared from primary amines in high yields by metal‐free diazo transfer with 2‐azido‐1,3‐dimethylimidazolinium hexafluorophosphate, which is a stable, crystalline solid that easy to handle.

Organic azides were prepared from primary amines in high yields by a metal free diazo-transfer reaction using 2-azido-1,3-dimethylimidazolinium hexafluorophosphate (ADMP), which is safe and stable crystalline. The choice of base was important the reaction. In general, 4-(N,N-dimethyl)aminopyridine (DMAP) efficient, but stronger such as alkylamine or DBU more appropriate for nucleophilic amines. X-ray single crystal structural analysis geometry optimization density functional theory...

We have developed the diazo-transfer of 2-azido-1,3-dimethylimidazolinium salts to 1,3-dicarbonyl compounds. 2-Azido-1,3-dimethylimidazolinium chloride (ADMC) was prepared by N-nitrosation N-aminoguanidine or reaction 2-chloro-1,3-dimethylimidazolinium (DMC) and sodium azide. The corresponding phosphate, ADMP, isolated as a crystal, found be stable safe reagent. Both ADMC ADMP reacted with compounds under mild conditions give 2-diazo-1,3-dicarbonyl in high yields, which are easily because...

Pd(OAc)2 was found to be an efficient catalyst for the macrocyclization of 1,2-diazonaphthoquinones and cyclic ethers. This transformation serves as method synthesis protected 1,2-naphthalenediols.

A cyclic naphthalene diimide (cyclic NDI, 1), carrying a benzene moiety as linker chain, was synthesized and its interaction with G-quadruplex DNAs of a-core a-coreTT human telomeric DNA, c-kit c-myc DNA sequence at promoter region, or thrombin-binding aptamer (TBA) studied based on UV-VIS circular dichroism (CD) spectroscopic techniques, thermal melting temperature measurement, FRET-melting assay. The spectra showed that 1 induced the formation different types structure. Compound bound to...

The β-hetero-substituted vinylphosphonates 1a−c on treatment with LDA or LTMP were readily lithiated at the α-position of phosphono group, and resulting α-lithiovinylphosphonates trapped various electrophiles to afford corresponding α-functionalized 2−14 in 55−96% yields. Friedel−Crafts reaction α-(silyl)- α-(germyl)phosphonoketene dithioacetals 2, 9, 4 acid chlorides gave α-acylated phosphonoketene 15−19 53−91% palladium-catalyzed cross-coupling β-ethoxy-α-(tributylstannyl)vinylphosphonate...

Direct synthesis of organic azides from alcohols was developed. Azide transfer 2-azido-1,3-dimethylimidazolinium hexafluorophosphate (ADMP) to proceeds give the corresponding under mild reaction conditions, which were easily isolated because byproducts are highly soluble in water.

An efficient synthetic method for the synthesis of diazo­naphthoquinones from naphthols is described. A variety were synthesized corresponding by diazo transfer with 2-azido-1,3-dimethylimidazolinium chloride prepared reaction 2-chloro-1,3-dimethylimidazorinium and sodium azide.

The generation of several α-phosphono-substituted vinyl carbanions is described. α-phosphonovinyl have been used to afford versatile vinylphosphonate reagents capable a wide range synthetic transformations.

Diazo transfer from 2-azido-1,3-dimethylimidazolinium chloride to 1,3-dicarbonyl compounds has been developed. The ­reaction proceeds under mild conditions give 2-diazo-1,3-dicarbonyl in high yields, which are easily isolated because the by-products highly soluble water.

Abstract Pd(II)-catalyzed formal O–H insertion reaction of diazonaphthoquinones to acetic acid proceeded afford 1,2-naphthalenediol monoacetates. In the presence lithium halides, halonaphthols were obtained under conditions.

A long-term air-stable n-type organic semiconductor, 2,5-difluoro-1,4-phenylene-bis{2-[4-(trifluoromethyl)phenyl]acrylonitrile}, was synthesized by a high-yield simple procedure of Knoevenagel condensation with aldehyde and acetonitrile derivatives. fabricated thin-film transistor (OTFT) using this compound exhibited good n-channel OTFT properties high electron mobility 0.17 cm2 V–1 s–1 an on/off current ratio 106 under both vacuum ambient air operation. After storage in for 1 year, stored...

gem-Difluoroolefins bearing homoallylic tosylamido, hydroxy, or mercapto groups undergo intramolecular nucleophilic substitution of the nitrogen, oxygen, sulfur with loss fluorine via a 5-endo-trig process, leading to 2-fluoro-2-pyrrolines, 5-fluoro-2,3-dihydrofurans, -thiophenes in high yields.

Abstract 2-Tributylstannyl-1,3-dithianes and 1-(tributylstannyl)alkyl sulfides are oxidized with ammonium hexanitratocerate(IV) or ferrocenium hexafluorophosphate to generate their cation radicals, which dissociate into the carbocations tributylstannyl radical. The thus generated react olefinic nucleophiles afford corresponding addition products in good yield.