1095239-01-2Relevant academic research and scientific papers
Synthesis of macrocyclic trypanosomal cysteine protease inhibitors
Chen, Yen Ting,Lira, Ricardo,Hansell, Elizabeth,McKerrow, James H.,Roush, William R.
supporting information; experimental part, p. 5860 - 5863 (2009/05/31)
The importance of cysteine proteases in parasites, compounded with the lack of redundancy compared to their mammalian hosts makes proteases attractive targets for the development of new therapeutic agents. The binding mode of K11002 to cruzain, the major cysteine protease of Trypanosoma cruzi was used in the design of conformationally constrained inhibitors. Vinyl sulfone-containing macrocycles were synthesized via olefin ring-closing metathesis and evaluated against cruzain and the closely related cysteine protease, rhodesain.
Catalytic asymmetric allylation of aldehydes using the chiral (salen)chromium(III) complexes
Kwiatkowski, Piotr,Cha?adaj, Wojciech,Jurczak, Janusz
, p. 5116 - 5125 (2007/10/03)
The enantioselective addition of allylstannanes to glyoxylates and glyoxals, as well as simple aromatic and aliphatic aldehydes, catalyzed by chiral (salen)Cr(III) complexes, has been studied. The reaction proceeded smoothly for the reactive 2-oxoaldehydes and allyltributyltin in the presence of small amounts (1-2 mol %) of (salen)Cr(III)BF4 (1b) under mild, undemanding conditions. However, in the case of other simple aldehydes, the use of high-pressure conditions is required to obtain good yields. Classic chromium catalyst 1b, easily prepared from the commercially available chloride complex 1a, affords homoallylic alcohols usually in good yield and with enantiomeric purity of 50-79% ee. The stereochemical results are rationalized on the basis of the proposed model.
Enantioselective allylation of alkyl glyoxylates catalyzed by (salen)chromium(III) complexes
Kwiatkowski, Piotr,Cha?adaj, Wojciech,Jurczak, Janusz
, p. 5343 - 5346 (2007/10/03)
The enantioselective addition of allylstannanes and allylsilanes to alkyl glyoxylates of type 1, catalyzed by chiral (salen)Cr(III) complexes 3, has been studied. We have found that the reaction proceeded smoothly for low loading (1-2mol%) of (1R,2R)-(sal
