Reference of 135861-56-2, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 135861-56-2, Name is (1R)-1-((4R,4aR,8aS)-2,6-Bis(3,4-dimethylphenyl)tetrahydro-[1,3]dioxino[5,4-d][1,3]dioxin-4-yl)ethane-1,2-diol, SMILES is O[C@@H]([C@@H]1[C@@](OC(C2=CC=C(C)C(C)=C2)OC3)([H])[C@@]3([H])OC(C4=CC=C(C)C(C)=C4)O1)CO, belongs to chiral-nitrogen-ligands compound. In a article, author is Latli, Bachir, introduce new discover of the category.
Synthesis of highly potent lymphocyte function-associated antigen-1 antagonists labeled with carbon-14 and with stable isotopes, part 3
The drug candidates (2) and (3) are highly potent LFA-1 inhibitors. They were efficiently prepared labeled with carbon-14 using a palladium-catalyzed carboxylation of an iodo-precursor (5) and sodium formate-C-14 to afford acid [C-14]-(6), which was coupled via an amide bond to chiral amines (7) and (8) in 52% and 48% overall yield, respectively, and with specific activities higher than 56 mCi/mmol and radiochemical purities of 99%. For stable isotopes synthesis, the amine [H-2(8)]-(7) was synthesized in three steps from 2-cyanopyridine-H-2(4) using Kulinkovich-Szymonik aminocyclopropanation, followed by coupling to L-alanine-2,3,3,3-H-2(4)-N-t-BOC, and then removal of the BOC-protecting group. Amide bond formation with acid (6) gave [H-2(8)]-(2) in 36% overall yield. The amine [C-13(4),N-15]-(8) was obtained in two steps using L-threonine-C-14(4),N-15 and then coupled to acid [C-13]-(6) to give [C-13(5),N-15]-(3) in 56% overall yield.
Reference of 135861-56-2, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 135861-56-2.
Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis¡ªI. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
,Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis