An effective approach to the enantiomers of alicyclic β-aminonitriles by using lipase catalysis
摘要:
Lipase-catalyzed N-acylations of racemic cis- and trans-2-aminocyclopentane- (and cyclohexane-) carbonitriles with 2,2,2-trifluoethyl butanoate in tert-butyl methyl ether (TBME) and in room-temperature ionic liquids (RTILs) were studied. The racemates were effectively resolved (E > 200) on a preparative scale by lipase PS-C II (lipase from Burkholderia cepacia) in TBME, resulting in two enantiomers in their enantiopure forms at 50% conversion. The reactions in RTILs with Novozym 435 (Candida antarctica lipase B) were slow and proceeded with low enantio selectivity. (c) 2005 Elsevier Ltd. All rights reserved.
(Ethylene)-(propylene) - triaminepentaacetic acid derivatives, process for their production, and their use for the production of pharmaceutical agents
申请人:Schering AG
公开号:US20030194371A1
公开(公告)日:2003-10-16
The invention relates to (ethylene)-(propylene)-triaminepentaacetic acid derivatives that are substituted on both the ethylene bridge and the propylene bridge, as well as conjugates of these compounds with biomolecules. The compounds and conjugates are suitable as agents for NMR diagnosis and radiodiagnosis as well as for radiotherapy.
New platinum (IV) complexes are now provided, which exhibit antitumor activity as shown by the tests on mouse leukemia, L-1210 cell in mice. These new platinum (IV) complexes contain, 1,2-cyclohexanediamine or 2-(aminomethyl)cylclohexyl-amine as a ligand.
Novel platinum(II)-steroid complexes are now provided, which exhibit antitumor activities as shown by tests on mouse leukemia, L-1210 cells in mice. These novel platinum(II)-steroid complexes contain a 1,2-cyclohexanediamine, a 2-(aminomethyl)cyclohexylamine, an ethylenediamine or NH₃- groups as a ligand or ligands.
(Ethylene)-( propylene)-triaminepentaacetic acid derivatives, process for their production, and their use for the production of pharmaceutical agents
申请人:——
公开号:US20040258620A1
公开(公告)日:2004-12-23
The invention relates to a novel class of ligands, complexes comprising such ligands and a metal ion, and adducts of these metal complexes and a macromolecule. Pharmaceutical compositions and methods of making and using the ligand-metal complexes are also described. The invention also relates to the use of macromolecular adducts for enhancement of diagnostic imaging. In particular, the invention relates to (ethylene)-(propylene)-triaminepentaacetic acid (EPTPA) derivatives, a process for their production, and their use for the production of pharmaceutical agents for NMR diagnosis or radiodiagnosis or radiotherapy.