Highly Regioselective N-2 Arylation of 4,5-Dibromo-1,2,3-triazole: Efficient Synthesis of 2-Aryltriazoles
摘要:
Reaction of 4,5-dibromo-1,2,3-triazole with electron-deficient aromatic halides in the presence of potassium carbonate in DMF produces the corresponding 2-aryl-4,5-dibromotriazoles with high regioselectivity. Subsequent debromination of these triazoles by hydrogenation furnishes 2-aryltriazoles in excellent yields. Overall, this two-step process provides an efficient access to 2-aryl-1,2,3-triazoles.
[EN] SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT<br/>[FR] COMPOSÉS CYCLOPROPYLE SUBSTITUÉS, COMPOSITIONS CONTENANT DE TELS COMPOSÉS ET PROCÉDÉS DE TRAITEMENT
申请人:MERCK SHARP & DOHME
公开号:WO2011019538A1
公开(公告)日:2011-02-17
Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
[EN] HETEROARYL-SUBSTITUTED SPIROCYCLIC DIAMINE UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE<br/>[FR] MODULATEURS D'AMIDE D'ACIDE GRAS HYDROLASE DE TYPE DIAMINE URÉE SPIROCYCLIQUE SUBSTITUÉE PAR UN GROUPE HÉTÉROARYLE
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2010141817A1
公开(公告)日:2010-12-09
Certain heteroaryl-substituted spirocyclic diamine urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).
[EN] ARYL-SUBSTITUTED HETEROCYCLIC UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE<br/>[FR] MODULATEURS HETEROCYCLIQUES A BASE D'UREE A SUBSTITUTION ARYLE DE L'HYDROLASE DES AMIDES D'ACIDES GRAS (FAAH)
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2010141809A1
公开(公告)日:2010-12-09
Certain aryl-substituted heterocyclic urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).
SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
申请人:Wood Harold B.
公开号:US20120142706A1
公开(公告)日:2012-06-07
Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
HETEROARYL-SUBSTITUTED SPIROCYCLIC DIAMINE UREA MODULATORS OF FATTY ACID AMIDE HYDROLASE
申请人:Breitenbucher J. Guy
公开号:US20120083476A1
公开(公告)日:2012-04-05
Certain heteroaryl-substituted spirocyclic diamine urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, energy metabolism disorders, and movement disorders (e.g., multiple sclerosis).