Metal-Free TEMPO-Promoted C(sp3)–H Amination To Afford Multisubstituted Benzimidazoles
摘要:
An efficient TEMPO-air/cat. TEMPO-O-2 oxidative protocol was developed to synthesize multisubstituted or fused tetracyclic benzimidazoles via a metal-free oxidative C-N coupling between the sp(3) C-H and free N-H of readily available N-1-benzyl/alkyl-1,2-phenylenediamines.
[EN] QUINOXALINONE DERIVATIVES AS INSULIN SECRETION STIMULATORS, METHODS FOR OBTAINING THEM AND USE THEREOF FOR THE TREATMENT OF DIABETES<br/>[FR] DÉRIVÉS DE QUINOXALINONE COMME STIMULATEURS DE LA SÉCRÉTION D'INSULINE, LEURS PROCÉDÉS D'OBTENTION ET LEUR UTILISATION POUR LE TRAITEMENT DU DIABÈTE
申请人:MERCK PATENT GMBH
公开号:WO2009109258A1
公开(公告)日:2009-09-11
The present invention relates to quinoxalinone derivatives of formula (I), wherein R1, R2, R3, R4, R5 and R6 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these quinoxalinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated. Other preferred compounds are compounds of general formula (I), wherein R1, R2, R3, R4, R5 and R6 can be optionally substituted by one or more groups selected from Z.
THE CONDENSATION OF PHOSPHONOTHIOIC AND PHOSPHONIC DICHLORIDES WITH <i>o</i>-DIAMINES
作者:Ralph L. Dannley、Arturs Grava
DOI:10.1139/v65-469
日期:1965.12.1
dichlorides, and phenylenediamines containing electron-donating substituents are more reactive than those containing electron-withdrawing substituents. The diazaphosphole 2-oxides undergo hydrolysis or alcoholysis of only one of the amide groups under mild conditions. The 2-sulfides are much more resistant to hydrolysis than the 2-oxides. The 2-sulfides are converted to the N-methyl derivatives by dimethyl
developed one‐step protocols for the preparation of a large selection of α‐aminocyclopropyl ketones or benzo[d]imidazoles, by reacting 2‐substituted‐2‐hydroxycyclobutanones with aryl amines or o‐phenylenediamines, respectively. In most case the reactions proceed at room temperature and are catalyst‐free. The formation of benzo[d]imidazoles is rationalized in terms of an unusual ring‐closure/ring‐fission process
The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
Imidoyl dichlorides as new reagents for the rapid formation of 2-aminobenzimidazoles and related azoles
作者:Julie A. Pollock、Sung Hoon Kim、John A. Katzenellenbogen
DOI:10.1016/j.tetlet.2015.09.076
日期:2015.10
yields. The ability to incorporate various protecting groups makes the imidoyl dichloride reagent amenable to a large number of syntheses. The reagent is applied to the total synthesis of the 2-aminobenzimidazole containing carcinogen, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP), from 2-chloro-3-nitropyridine in >60% yield in 6 steps.
提出了在室温下有效合成五元和六元唑的试剂的开发。合成了多种取代的2-氨基苯并咪唑,收率良好至优异。掺入各种保护基的能力使亚氨酰二氯化物试剂适合于大量合成。该试剂可用于由> 60的2-氯-3-硝基吡啶全合成含2-氨基苯并咪唑的致癌物2-氨基-1-甲基-6-苯基咪唑并[4,5- b ]吡啶(PhIP) 6个步骤中的%收率。