147878-72-6Relevant articles and documents
I-Pr2NMgCl·LiCl Enables the Synthesis of Ketones by Direct Addition of Grignard Reagents to Carboxylate Anions
Colas, Kilian,Dos Santos, A. Catarina V. D.,Mendoza, Abraham
supporting information, (2019/10/08)
The direct preparation of ketones from carboxylate anions is greatly limited by the required use of organolithium reagents or activated acyl sources that need to be independently prepared. Herein, a specific magnesium amide additive is used to activate and control the addition of more tolerant Grignard reagents to carboxylate anions. This strategy enables the modular synthesis of ketones from CO2 and the preparation of isotopically labeled pharmaceutical building blocks in a single operation.
Selective angiotensin II AT2 receptor agonists with reduced CYP 450 inhibition
Mahalingam,Wan, Yiqian,Murugaiah,Wallinder, Charlotta,Wu, Xiongyu,Plouffe, Bianca,Botros, Milad,Nyberg, Fred,Hallberg, Anders,Gallo-Payet, Nicole,Alterman, Mathias
experimental part, p. 4570 - 4590 (2010/09/12)
Structural alterations to the benzylic position of the first drug-like selective angiotensin II AT2 receptor agonist (1) have been performed, with the emphasis to reduce the CYP 450 inhibitory property of the initial structure. The imidazole moiety, responsible for the CYP 450 inhibitory effect in 1, was replaced with various heterocycles. In addition, the modes of attachment of the heterocycles, that is, carbon versus nitrogen attachment, and introduction of carbonyl functionalities to the benzylic position have been evaluated. In all the three series, AT2 receptor ligands with affinity in the lower nanomolar range were identified. None of the analogues, regardless of the substituents, exhibited any affinity for the AT1 receptor. Compounds with substantially reduced inhibition of the CYP 450 enzymes were obtained. Among them the compound 60 was found to induce neurite elongation in NG 108-15 cells and served as potent AT2 selective agonist.
NEW TRICYCLIC ANGIOTENSIN II AGONISTS
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Page 46, (2010/02/07)
There is provided compounds of formula (I), wherein the dotted lines, XI, X2, X3, X4, A, YI, Y2, Y3, Y4, ZI, Z2, R2 and R3