Stereoselective chemoenzymatic synthesis of both enantiomers of protected 4-amino-2-pentanone
An acetal protected 4-amino-2-pentanone was synthesised by two different routes in 10 and seven steps, respectively, the key step being a microbiological reduction. Both enantiomers of the amine were obtained enantiomerically pure.
Besse, Pascale,Ciblat, Stephane,Canet, Jean-Louis,Troin, Yves,Veschambre, Henri
MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS AND USES THEREOF
The present disclosure describes novel TRK kinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such TRK kinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described.
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Paragraph 256
(2019/05/30)
Synthesis and in vitro sodium channel blocking activity evaluation of novel homochiral mexiletine analogs
New chiral mexiletine analogs were synthesized in their optically active forms and evaluated in vitro as use-dependent blockers of skeletal muscle sodium channels. Tests carried out on sodium currents of single muscle fibers of Rana esculenta demonstrated