Bioorganic & Medicinal Chemistry Letters 2004-02-23

Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.

Jiabing Wang, Michael J Breslin, Paul J Coleman, Mark E Duggan, Cecilia A Hunt, John H Hutchinson, Chih-Tai Leu, Sevgi B Rodan, Gideon A Rodan, Le T Duong, George D Hartman

文献索引:Bioorg. Med. Chem. Lett. 14 , 1049, (2004)

全文:HTML全文

摘要

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 tetrahydro-[1,8]naphthyridine decreased potency while electron-donating groups enhanced potency.


相关化合物

  • 5-溴-2-甲氧基吡啶

相关文献:

An efficient synthesis of an alphavbeta3 antagonist.

2004-03-19

[J. Org. Chem. 69 , 1959-1966, (2004)]

[Tetrahedron Asymmetry 14 , 3469, (2003)]

The 1,3-Diaminobenzene-Derived Aminophosphine Palladium Pincer Complex {C6H3[NHP(piperidinyl)2]2Pd(Cl)}-A Highly Active Suzuki-Miyaura Catalyst with Excellent Functional Group Tolerance. Bolliger JL and Frech CM.

[Adv. Synth. Catal. 352(6) , 1075-1080, (2010)]

Functionalized pyridylboronic acids and their Suzuki cross-coupling reactions to yield novel heteroarylpyridines Parry PR, et al.

[J. Org. Chem. 67(21) , 7541-7543, (2002)]

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.

[Org. Process Res. Dev. 11(5) , 899-902, (2007)]

更多文献...