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1.
Bioorg Med Chem Lett ; 29(14): 1737-1745, 2019 07 15.
Article in English | MEDLINE | ID: mdl-31122869

ABSTRACT

The discovery, design and synthesis of a new series of GSMs is described. The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus. The exploration of this series has led to compound 26-S which combined high in vitro and in vivo potency with an acceptable drug-like profile.


Subject(s)
Amyloid Precursor Protein Secretases/metabolism , Indoles/chemical synthesis , Drug Design , Humans , Structure-Activity Relationship
2.
Chem Commun (Camb) ; (14): 1689-91, 2008 Apr 14.
Article in English | MEDLINE | ID: mdl-18368166

ABSTRACT

A new approach to the synthesis of pyrimidines and cyclopentenones is described. The method exploits the reactivity of alpha,beta-unsaturated acetals with aromatic nitriles in the presence of the Schlosser's superbase LIC-KOR.


Subject(s)
Acetals/chemistry , Butanes/chemistry , Cyclopentanes/chemical synthesis , Ethyl Ethers/chemistry , Imines/chemical synthesis , Lithium/chemistry , Nitriles/chemistry , Potassium/chemistry , Pyrimidines/chemical synthesis , Cyclopentanes/chemistry , Imines/chemistry , Molecular Structure , Pyrimidines/chemistry
3.
J Org Chem ; 69(16): 5187-95, 2004 Aug 06.
Article in English | MEDLINE | ID: mdl-15287760

ABSTRACT

The Boehringer-Ingelheim phosphinoimidazoline (BIPI) ligands were applied to the formation of chiral quaternary centers in the asymmetric Heck reaction. Several different substrates were examined in detail, using more than 70 members of this new ligand class. Hammett relationships were determined through systematic variation of the ligand electronics. All substrates showed essentially the same Hammett behavior, where enantioselectivity increased as the ligands were made more electron-deficient. Ligand optimization has led to catalysts which give the highest enantioselectivities reported to date for these difficult systems.

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