A building block for the β-alanine moiety of an αvβ3 antagonist[1][2] and for the synthesis of a potent and selective somatostatin sst3 receptor antagonist.[3]
The Journal of organic chemistry, 69(6), 1959-1966 (2004-04-03)
A practical preparation of an alpha(v)beta(3) antagonist is reported. The antagonist consists of three key components, a tetrahydronaphthyridine moiety, a beta-alanine moiety, and a central imidazolidone moiety. The tetrahydronaphthyridine component was prepared using two different methods, both of which relied
Tetrahedron Asymmetry, 14, 3469-3469 (2003)
Negishi Cross-Coupling Reactions Catalyzed by an Aminophosphine-Based Nickel System: A Reliable and General Applicable Reaction Protocol for the High-Yielding Synthesis of Biaryls.
Gerber R and Frech CM.
Chemistry (Weinheim An Der Bergstrasse, Germany), 17(42), 11893-11904 (2011)
A scaleable synthesis of methyl 3-amino-5-(4-fluorobenzyl)-2-pyridinecarboxylate. Organic Process Research & Development 11.5 (2007): 899-902
Boros EE, et al.
Organic Process Research & Development, 11(5), 899-902 (2007)
A series of 3-substituted tetrahydro-[1,8]naphthyridine containing alpha(v)beta(3) antagonists was prepared. A comparison of their in vitro IC(50) values to the electron properties of the 3-substituents revealed a good linear Hammett correlation (rho=-1.96, R(2)=0.959). Electron-withdrawing groups at the 3-position of the
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