Reactive Site Cleavage, Thermodynamic Control Resynthesis, and Properties of Chemically Derivatized Trypsin-Kallikrein-Inhibitors

Author(s):  
H. Tschesche ◽  
H. Jering ◽  
G. Schorp ◽  
T. Dietl
Author(s):  
Gudrun A. Hutchins

In order to optimize the toughening effect of elastomers in engineering polymers, it is necessary to characterize the size, morphology and dispersion of the specific elastomer within the polymer matrix. For unsaturated elastomers such as butadiene or isoprene, staining with osmium tetroxide is a well established procedure. The residual carbon-carbon double bond in these materials is the reactive site and forms a 1,2-dilato complex with the OsO4. Incorporation of osmium tetroxide into the elastomer not only produces sufficient contrast for TEM, but also crosslinks the elastomer sufficiently so that ultramicrotomy can be accomplished at room temperature with minimal distortion.Blends containing saturated elastomers such as butyl acrylate (BA) and ethylene propylene diene monomer (EPDM) cannot be stained directly with OsO4 because effective reaction sites such as C=C or -NH2 are not available in sufficient number. If additional reaction sites can be introduced selectively into the elastomer by a chemical reaction or the absorption of a solvent, a modified, two-step osmium staining procedure is possible.


2020 ◽  
Author(s):  
Rui Guo ◽  
Xiaotian Qi ◽  
Hengye Xiang ◽  
Paul Geaneoates ◽  
Ruihan Wang ◽  
...  

Vinyl fluorides play an important role in drug development as they serve as bioisosteres for peptide bonds and are found in a range of biologically active molecules. The discovery of safe, general and practical procedures to prepare vinyl fluorides remains an important goal and challenge for synthetic chemistry. Here we introduce an inexpensive and easily-handled reagent and report simple, scalable, and metal-free protocols for the regioselective and stereodivergent hydrofluorination of alkynes to access both the E and Z isomers of vinyl fluorides. These conditions were suitable for a diverse collection of alkynes, including several highly-functionalized pharmaceutical derivatives. Mechanistic and DFT studies support C–F bond formation through a vinyl cation intermediate, with the (E)- and (Z)-hydrofluorination products forming under kinetic and thermodynamic control, respectively.<br>


1989 ◽  
Vol 264 (6) ◽  
pp. 3066-3071
Author(s):  
K Skriver ◽  
E Radziejewska ◽  
J A Silbermann ◽  
V H Donaldson ◽  
S C Bock
Keyword(s):  

1993 ◽  
Vol 268 (31) ◽  
pp. 23626-23633 ◽  
Author(s):  
N.M. Schechter ◽  
L.M. Jordan ◽  
A.M. James ◽  
B.S. Cooperman ◽  
Z.M. Wang ◽  
...  

1980 ◽  
Vol 255 (9) ◽  
pp. 3820-3823
Author(s):  
J.B. Howard ◽  
M. Vermeulen ◽  
R.P. Swenson

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