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N-alkyl-2,2-dihaloamides were efficiently prepared by amino-de-alkoxylation of methyl 2,2-dihalocarboxylates, at room temperature without solvents and promoters. Excellent yields of anilides were obtained after addition of AlCl 3 .
ortho-Phenylenediammes react with formaldehyde and cyclopentadiene in acetonitrile in the presence of trifluoroacetic acid to give two types of product. With excess formaldehyde and cyclopentadiene pentacyclic diamines are obtained. Tricyclic diamines are favoured when less formaldehyde is used....
A series of new N-(pyridylmethyl)azinium salts have been synthesized from 2, 4, 6-triphenylpyrylium tetrafluoroborate. Generation of azinium N-ylides in the presence of base, has been proved by reactions with electrophiles, such as carbon disulphide, phenyl isothiocyanate and with acetylene...
Fractions from Larrea tridentata with anti-HIV-1 activity (specifically, inhibition of HIV Tat transactivation) were analyzed by GC/MS and NMR and found to contain lignans 1a-i and 2a-d . Assay-guided purification by countercurrent chromatography established 1g (mal.4) to be especially active....
Phosphorylation of N-alky lated imidazoles and benzimidazoles at C-2 by CH 3 POCl 2 , PhPOCl 2 -POCl 3 in pyridine-triethylamine solution is described. The formed heteroaryl-substituted phosphinic or phosphonic acid chlorides were transformed without isolation into the corresponding phosphinic...
The synthesis of 3′-deoxy-3′-C-hydroxymethyl-aldopentopyranosyl nucleosides using an intramolecular radical C-C bond formation reaction is described. This method gives good results for the synthesis of thymine and adenine nucleosides, but not for cytosine and guanine nucleosides. Dependent on...
The reactions of vinyl sulfoximines ( 1a-e ) with C , N -diphenylnitrone ( 2 ) are highly regioselective and give only 4-sulfonimidoyl-isoxazolidine cycloadducts. These reactions proceed with modest π -facial diastereoselectivity with respect to the dipolarophile. The stereochemical outcome of...
Enantiopure N -and/or C -protected homo -β-amino acids are prepared readily and in good yields from N -protected α-amino acids with the same side chain, via reduction of the carboxyl function and conversion of the resulting N -protected β-amino alcohol into the corresponding β-amino iodide...
In the presence of Lewis acid, such as SbCl 5 , SbCl 6 ·NAr 3 or Cu(OTf) 2 , difluorovinyl methyl ether (1,1-difluoro-2-methoxy-1-alkene) 1 reacted with carbonyl compounds to give O -methylated aldol-type products 3 in good yields, while Lewis acid, such as TMSOTf, TiCl 4 or BF 3 ·Et 2 O, did...
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