Free radical fluoroalkylation of terminal alkenes and alkynes with iododifluoromethanesulfonamides has been successfully achieved.It was found that both the catalytic amount of sodium dithionite (Na2S2O4) and the stoichiometric amount of triethylborane (Et3B)/air can efficiently initiate the current free-radical atom transfer reaction.
ZHU JieMing,WANG Fei & HU JinBo CAS Key Laboratory of Organofluorine Chemistry
3-Deazaneplanocin A （3-DNPA, 2）, an antiviral and antitumor agent, has been synthesized in an optimized procedure in 10 steps, with an increased overall yield of 11.2%. Started from 2,4-dihyroxyl-3-nitropyridine, reduction of nitro group and ring closure of imidazole were carried out in one pot, without the separation of diaminopyridine （10）, to give 3-deazapurine （11）. Moreover, the conversion of 6-chloro-3-deazapurine （12） to 6-amino-3-deazapurine （13） and the synthesis of N^6,N^6,N9-tris-Boc-3- deazadenine （16） was promoted by microwave-aid method. Compound 16 benefited the formation of N9 isomer of 3-DNPA in Mitsunobu reaction.
Difluoromethyltri（n-butyl）ammonium chloride 1 was found to be an effective difluorocarbene reagent for O-, S-, N-, C-difluoromethylation under basic conditions. It is particularly remarkable that, when only 1.2 equivalent of reagent 1 was used, the difluoromethylated products were obtained in moderate to excellent yields.
Three dinucleotides containing L-isonucleosides at 5＇-end were synthesized by an elegant phosphoramidite one-pot method. Their binding modes with HIV integrase were simulated and their anti-HIV activities in pseudotyped virus system were examined.
Difluoromethylene group(CF2) can act as an isopolar-isosteric substitute for oxygen,and replacement of the pho...
Zhang Feng,Fei Chen,and Xingang Zhang~* Key Laboratory of Organofluorine Chemistry,Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences,345 Lingling Road,Shanghai 200032,China
＜正＞Sulfoximines（sometimes also called sulfoximides）are structurally unique derivatives of sulfones,which are a...
Jinbo Hu,Wei Zhang,Xiao Shen and Tao Luo Key Laboratory of Organofluorine Chemistry,Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences,345 Ling-Ling Road,Shanghai 200032,China
