2a,4-Disubstituted 2,2a,3,4-tetrahydro-2-phenyl-1H-azeto[2,1-d][1,5]benzothiazepin-1-ones, as well as 2-substi- tuted 2,3-dihydro-3-phenylacetyl-2-styryl-benzothiazoles and 4a,6-disubstituted 3-benzyl-4a,5-dihydro-2-phenyl- 1H,6H-[1,3]oxazino[2,3-d][1,5]benzothiazepin-1-ones, were obtained from the reaction of 2,4-disubstituted 2,3-dihydro-1,5-benzothiazepines with phenylacetyl chloride in the presence of triethylamine. The mechanism for the formation of 4a,5-dihydro-1H,6H-[1,3]oxazino[2,3-d][1,5]benzothiazepin-1-ones, 2,3-dihydro-1,3-oxazin-4-one derivatives, was suggested.
The mass spectrometric fragmentation of 1,8-bis [ 4-substituted （oxazolin-2-yl） ] anthracenes （AnBOXes） was investigated by using mass-analyzed ion kinetic energy spectrometry under electron-impact ionization conditions. All the compounds could undergo a ring contraction by the loss of an RCH = CH2 molecule to form 1-oxazirinyl-8-（oxazolin- 2-yl） anthracene ions, which could further lose an R radical, followed by the loss of oxazoline. These ions could also eliminate an R radical and subsequently undergo ring-contraction rearrangements to lose a CHCH2O fragraent and an epoxide molecule, respectively. The ions that are formed could further lose CHCH2O and CH2 = CH fragments. Several ring-contraction rearrangements of the oxazoline ring were observed under electron-impact ionization conditions.
An intermolecular phenolic hydroxy methylation occurring between chiral N,N'-bis(2-hydroxyphenyl)-2,2-di- methyl-1,3-dioxolane-4,5-dicarbamide and co-crystallized methanol under electron impact ionization conditions was observed. The result was confirmed by X-ray diffraction structural ananlysis of a co-crystalline of (R,R)-enantiomer and methanol.
Phosphonate and phosphonamidate peptides are phosphorus analogues of natural peptides. They have been great used as stable mimetics of tetrahedral transition states as enzyme inhibitors and as haptens for catalytic antibody research in recent years. Although several methods are available for the preparation of phosphonate peptides and phosphonamidate peptides, all of them use phosphonic acid derivatives as starting materials. The overall yields from the synthesis of phosphonic acid derivatives to desired peptides are not satisfactory in most cases.……
XU Jia-Xi FU Nan-Yan GAO Yuan-He ZHNAG Qi-Han DUAN Li-Fang
