Synthesis of the GPR40 partial agonist MK-8666 through a kinetically controlled dynamic enzymatic ketone reduction
A scalable and efficient synthesis of the GPR40 agonist MK-8666 was developed from a simple pyridine building block. The key step to set the stereochemistry at two centers relied on an enzymatic dynamic kinetic reduction of an unactivated ketone. Directed
Hyde, Alan M.,Liu, Zhijian,Kosjek, Birgit,Tan, Lushi,Klapars, Artis,Ashley, Eric R.,Zhong, Yong-Li,Alvizo, Oscar,Agard, Nicholas J.,Liu, Guiquan,Gu, Xiuyan,Yasuda, Nobuyoshi,Limanto, John,Huffman, Mark A.,Tschaen, David M.
supporting information
p. 5888 - 5891
(2016/11/29)
Platinum(II) Complexes of Functionalized Malonato Ligands: Unequivocal Synthesis, Interaction with a Tetradeoxyribonucleotide and Deoxyribonucleic Acid
The unequivocal syntheses of four cis-> complexes has been achieved, avoiding any interaction between the pendant carboxyl group and the platinum.The complexes have been characterized by elemental analysis, 13C NMR and FAB mass spectroscopy.Their interaction with a tetradeoxyribonucleotide d(T-G-G-T) (G = guanosine, T = ribosylthymine) and DNA (in vitro) has been investigated to show that they form adducts of the type 7,N7'>> as do the known therapeutically activeplatinum complexes.However, the presence of the free carbonyl function increases significantly the reactivity with respect to that of the non-functionalized malonato complexes >.
Laurent, Jean-Pierre,Morvan, Bernard
p. 2141 - 2146
(2007/10/02)
HIGHLY STEREOSELECTIVE RADICAL ADDITION TO A TRISUBSTITUTED ALKENE BY LOW TEMPERATURE PHOTOLYSIS OF THIOHYDROXAMIC ESTERS
Low temperature carbon radical addition to α,β-unsaturated amides of trans-2,5-dimethylpyrrolidine was achieved in high yield with high diastereoselectivity by photolysis of Barton esters.Use of an olefin substituted with three electron withdrawing groups
Scott, Daniel M.,McPhail, Andrew T.,Porter, Ned A.
p. 1679 - 1682
(2007/10/02)
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