- Photoinduced Deaminative Borylation of Alkylamines
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An operationally simple deaminative borylation reaction of primary alkylamines has been developed. The formation of electron-donor-acceptor complexes between N-alkylpyridinium salts and bis(catecholato)diboron enables photoinduced single-electron transfer and fragmentation to carbon-centered radicals, which are subsequently borylated. The mild conditions allow a diverse range of readily available alkylamines to be efficiently converted into synthetically valuable alkylboronic esters under catalyst-free conditions.
- Wu, Jingjing,He, Lin,Noble, Adam,Aggarwal, Varinder K.
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supporting information
p. 10700 - 10704
(2018/09/06)
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- Synthesis and antibacterial activity of 3-benzylamide derivatives as FtsZ inhibitors
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The emergence and spread of multidrug-resistant strains of the human pathological bacteria are generating a threat to public health worldwide. In the current study, a series of PC190723 derivatives was synthesized and investigated for their antimicrobial activity. The compounds exhibited good activity against several Gram-positive bacteria as determined by comparison of diameters of the zone of inhibition of test compounds and standard antibiotics. Compound 9 with a fluorine substitution on the phenyl ring showed the best antibacterial activity in the series against M. smegmatis with the zone ratio of 0.62, and against S. aureus with the zone ratio of 0.44. The results from this study indicate that based on the unique 3-methoxybenzamide pharmacophore, compound 9 may represent a promising lead candidate against Gram-positive bacteria that are worthy of further investigation
- Hu, Zhongping,Zhang, Shasha,Zhou, Weicheng,Ma, Xiang,Xiang, Guangya
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supporting information
p. 1854 - 1858
(2017/04/04)
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- Reactions of difluorocarbene with organozinc reagents
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Reactions of difluorocarbene with benzyl and alkylzinc halides leading to fluorinated organozinc species have been described. The generated α-difluorinated organozinc reagents are reasonably stable in solution and can be quenched with external electrophiles (iodine, bromine, proton), affording compounds containing the CF2 fragment.
- Levin, Vitalij V.,Zemtsov, Artem A.,Struchkova, Marina I.,Dilman, Alexander D.
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supporting information
p. 917 - 919
(2013/03/28)
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- Dual Bronsted acid/nucleophilic activation of carbonylimidazole derivatives
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Carbonylimidazole derivatives have been found to be highly active acylation reagents for esterification and amidation in the presence of pyridinium salts. These reactions are thought to involve both Bronsted acid and nucleophilic catalysis. This mode of activation has been applied to the synthesis of difficult to access oxazolidinones, as well as esters and amides. Finally, the use of pyridinium salts has been shown to accelerate the esterification of carboxylic acids with imidazole carbamates.
- Heller, Stephen T.,Fu, Tingting,Sarpong, Richmond
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supporting information; experimental part
p. 1970 - 1973
(2012/06/01)
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- Indium-catalyzed radical reductions of organic halides with hydrosilanes
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(Equation Presented) The In(OAc)3-catalyzed reaction of bromo- and iodoalkanes with PhSiH3 in THF at 70°C gave dehalogenated alkanes in good to high yields. In the presence of Et3B and air, the reduction proceeded smoothly at 30°C. When 2,6-lutidine and air were used as additives, the In(OAc)3-catalyzed system enabled an efficient reduction of simple and functionalized iodoalkanes in EtOH. Catalytic use of GaCl3 was found to be effective in the reduction of haloalkanes with poly(methylhydrosiloxane) (PMHS). These catalytic reductions probably involve a radical chain mechanism in which indium or gallium hydride species work as the actual reductants.
- Miura, Katsukiyo,Tomita, Mitsuru,Yamada, Yusuke,Hosomi, Akira
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p. 787 - 792
(2007/10/03)
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- One-pot synthesis of ω-bromoesters from aromatic aldehydes and diols using pyridinium hydrobromide perbromide
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A simple and efficient one-pot procedure has been developed for the synthesis of ω-bromoesters from aromatic aldehydes and diols in the presence of pyridinium hydrobromide perbromide (PHPB) and triethoxymethane in which aldehyde reacts first with diol and the product, cyclic acetal, reacts with PHPB to give the final product, ω-bromoesters.
- Aoyama, Tadashi,Takido, Toshio,Kodomari, Mitsuo
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p. 1989 - 1992
(2007/10/03)
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- 1-N-AMINOBENZIMIDAZOLE DERIVATIVES
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Provided are 1-N-aminobenzimidazole derivatives represented by the following formula (I): wherein R1 and R2 each represents a substituted or unsubstituted alkyl group or the like, R3, R5 and R6 each represents an alkyl group, alkoxy group, hydrogen atom or the like, R4 represents a substituted or unsubstituted alkyl group or the like, A represents a benzene ring or the like, B represents a hydrogen atom or the like, an n stands for an integer of from 0 to 2, or salts thereof; and medicines containing them. The compounds (I) according to the present invention do not bring about much individual differences in therapeutic effects despite the existence of individual differences in the CYP2C19 activity. At the same dose, they can hence bring about appropriate therapeutic effects for all patients. In addition, they are low in the risk of induction of an interaction or a cancer caused by induction of the CYP1A family. Accordingly, they are useful as peptic ulcer therapeutic agents which are safe and surely bring about therapeutic effects.
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- A facile synthesis of large extraannular-functionalized phenyl-ethynyl macrocycles containing m-terphenyl units
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(equation presented) Two large extraannular-functionalized phenyl-ethynyl macrocycles containing m-terphenyl units are described. The synthesis of the m-terphenyl building blocks is based on the transformation of pyrylium salts to arenes.
- Hoeger, Sigurd,Rosselli, Silvia,Ramminger, Anne-Desiree,Enkelmann, Volker
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p. 4269 - 4272
(2007/10/03)
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- A new synthetic method for haloalkyl carboxylic esters from the radical ring cleavage of cyclic acetals with haloform
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A one-pot reaction of cyclic acetals with haloform catalyzed by AIBN(2,2'-azobisisobutyronitrile) provides a novel convenient way to prepare directly haloalkyl carboxylic esters in good yields.
- Hai-Xia, Lin,Liang-Heng, Xu,Nai-Ju, Huang
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p. 303 - 306
(2007/10/03)
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- Synthesis of Nitriles from Haloesters, Haloketones and Haloethers
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The action of NaCN on haloesters, haloketones and haloethers has been studied.Haloesters wherein halogen and ester functions are located on adjacent carbon atoms, do not furnish the corresponding nitriles, whereas those with halogen and ester functions not located on adjacent carbon atoms, furnish the corresponding nitriles in good yields.The presence of hydroxy or ether function on the carbon adjacent to primary halide bearing carbon atom does not interfere in the reaction with cyanide. δ-Haloketones are transformed to ketonitriles, γ-Haloketones are transformed to cyclopropyl ketones and epoxyhalides to epoxynitriles.
- Talekar, D. G.,Joshi, P. L.,Ramaiah, P.,Rao, A. S.
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p. 145 - 151
(2007/10/02)
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