57724-90-0Relevant academic research and scientific papers
Photoinduced, copper-catalyzed alkylation of amides with unactivated secondary alkyl halides at room temperature
Do, Hien-Quang,Bachman, Shoshana,Bissember, Alex C.,Peters, Jonas C.,Fu, Gregory C.
supporting information, p. 2162 - 2167 (2014/03/21)
The development of a mild and general method for the alkylation of amides with relatively unreactive alkyl halides (i.e., poor substrates for S N2 reactions) is an ongoing challenge in organic synthesis. We describe herein a versatile transition-metal-catalyzed approach: in particular, a photoinduced, copper-catalyzed monoalkylation of primary amides. A broad array of alkyl and aryl amides (as well as a lactam and a 2-oxazolidinone) couple with unactivated secondary (and hindered primary) alkyl bromides and iodides using a single set of comparatively simple and mild conditions: inexpensive CuI as the catalyst, no separate added ligand, and C-N bond formation at room temperature. The method is compatible with a variety of functional groups, such as an olefin, a carbamate, a thiophene, and a pyridine, and it has been applied to the synthesis of an opioid receptor antagonist. A range of mechanistic observations, including reactivity and stereochemical studies, are consistent with a coupling pathway that includes photoexcitation of a copper-amidate complex, followed by electron transfer to form an alkyl radical.
Efficacy switching SAR of mGluR5 allosteric modulators: Highly potent positive and negative modulators from one chemotype
Sams, Anette Graven,Mikkelsen, Gitte Kobber?e,Brodbeck, Robbin M.,Pu, Xiaosui,Ritzén, Andreas
, p. 3407 - 3410 (2011/07/07)
A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, and the
INDENYL DERIVATIVES AND USE THEREOF FOR THE TREATMENT OF NEUROLOGICAL DISORDERS
-
Page/Page column 21, (2008/06/13)
The present invention relates to novel indenyl derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
P2x7 receptor antagonists for use in the treatment of inflammatory, immune or cardiovascular diseases
-
, (2008/06/13)
The invention provides piperidine compounds of general formula (I) in which A, B, X, Y, Z, R, R1 and R2 are as defined in the specification, their use as medicaments, compositions containing them and processes for their for their preparation.
