Organic Communications Articles
Issue: 1 January-March
Year: 2015 Volume: 8 Issue:1 January-March
1) Synthesis of chiral phosphonoacetamides and their toxic effects on paramecium sp
Three chiral phosphonoacetamides were prepared by an alternative method . For this purpose, 2-(diethoxyphosphoryl)acetic acid was prepared from ethyl 2-bromoacetate by treatment of P(OEt) 3 followed by saponification of the ester with K 2CO 3. BOP activated amidation of the 2-(diethoxyphosphoryl)acetic acid with (S)-amino acids gave the corresponding phosphonoaceteamides. Growth inhibition of two phosphonoacetamides on Paramecium sp. were studied.Keywords Paramecium sp Organophosphorus Phosphonoacetamide phosphorylation coupling reaction DETAILS PDF OF ARTICLE © 2015 ACG Publications. All rights reserved.
2) The first investigation of borane-unsaturated nucleoside reaction system
A novel synthetic approach is presented, involving unsaturated nucleoside hydroboration, with protected stavudine catalytically boronated with pinacolborane to several pinacolborane derivatives of stavudine or 2’,3’-dideoxythymidine. The products were converted to much more stable trifluoroborate derivatives that may be considered trifluoroboron analogues of nucleoside phosphates. The post-reaction mixture contained four isomers, being products of catalytic hydroboration, and two isomers, resulting from dehydrogenative borylation, each containing unsaturated 2’,3’-moiety. The new compounds were analyzed with NMR and LDI-HRMS methods.Keywords BNCT boron nucleoside boron nucleotide dehydrogenative borylation hydroboration NMR DETAILS PDF OF ARTICLE © 2015 ACG Publications. All rights reserved.
3) Synthesis and antioxidant activity of dioxazaphosphinin-2-ones
A simple and efficient synthesis of dioxazaphosphinin-2-ones has been developed by the cyclisation of 2-hydroxy-1,2-diphenylethanoneoxime with phosphorus oxychloride in the presence of triethylamine in dry THF to afford the corresponding monochloride. In the next step, subsequent reaction of monochloridewith different amines at 50-60 ˚C for 2-3 hours resulted in the formation of the title compounds (4a-j). The lead compounds were screened for their antioxidant activity.Keywords 2-hydroxy 1 2-diphenylethanoneoxime POCl 3 dioxazaphosphinin-2-ones Antioxidant activity DETAILS PDF OF ARTICLE © 2015 ACG Publications. All rights reserved.