( R )-3二甲氨基吡咯烷是合成药物巴氟替尼的关键手性中间体。本文以L-苹果酸为起始原料,经过环化、还原、过磺酰化、脱保护等反应合成了( R )-3-二甲氨基吡咯烷,总收率31.45%,其结构经 1 H NMR, 13 C NMR 和IR确证。并对关键中间体的...( R )-3二甲氨基吡咯烷是合成药物巴氟替尼的关键手性中间体。本文以L-苹果酸为起始原料,经过环化、还原、过磺酰化、脱保护等反应合成了( R )-3-二甲氨基吡咯烷,总收率31.45%,其结构经 1 H NMR, 13 C NMR 和IR确证。并对关键中间体的合成条件进行了优化。展开更多
The interactions between several peptides with low molecular weight (guest, NH2 Arg Arg Trp Trp H 2; NH2 Arg Trp Arg Trp H 3; NH2 Trp Arg Arg Trp H 4; NH2 Arg Arg Trp Trp Trp Trp H 5; NH2 Trp Trp Arg Arg Trp Trp H 6; ...The interactions between several peptides with low molecular weight (guest, NH2 Arg Arg Trp Trp H 2; NH2 Arg Trp Arg Trp H 3; NH2 Trp Arg Arg Trp H 4; NH2 Arg Arg Trp Trp Trp Trp H 5; NH2 Trp Trp Arg Arg Trp Trp H 6; NH2 Arg Arg Trp Trp Trp Trp Trp Trp H 7; NH2 Arg Arg Trp Trp Trp Trp Trp Trp Trp Trp H 8) and β cyclodextrin dimer (host, 1) bridged with the derivative of (1R, 3R) 1 aminocyclobutane cis 1,3 dicar boxylic acid were investigated by using fluorescence polarization method in buffer aqueous solution (pH 7.4) at 298K. The binding constants of the cyclodextrin dimer 1 to the guests 2 8 were determined. It was shown that there was a cooperative action of the two cavities of a cyclodextrin dimer in the binding of large substrates, and that the structure and properties of amino acid in the peptides played very important roles in the synergic complexation between host and guest.展开更多
文摘The interactions between several peptides with low molecular weight (guest, NH2 Arg Arg Trp Trp H 2; NH2 Arg Trp Arg Trp H 3; NH2 Trp Arg Arg Trp H 4; NH2 Arg Arg Trp Trp Trp Trp H 5; NH2 Trp Trp Arg Arg Trp Trp H 6; NH2 Arg Arg Trp Trp Trp Trp Trp Trp H 7; NH2 Arg Arg Trp Trp Trp Trp Trp Trp Trp Trp H 8) and β cyclodextrin dimer (host, 1) bridged with the derivative of (1R, 3R) 1 aminocyclobutane cis 1,3 dicar boxylic acid were investigated by using fluorescence polarization method in buffer aqueous solution (pH 7.4) at 298K. The binding constants of the cyclodextrin dimer 1 to the guests 2 8 were determined. It was shown that there was a cooperative action of the two cavities of a cyclodextrin dimer in the binding of large substrates, and that the structure and properties of amino acid in the peptides played very important roles in the synergic complexation between host and guest.
