Biphenyl versus Phenylpyridazine Derivatives: The Role of the Heterocycle in a Series of Acyl-CoA:Cholesterol Acyl Transferase Inhibitors
摘要:
A series of alkylamido- (1) and alkylaminobiphenyl (2) derivatives were synthesized as possible bioisosters of the reported ACAT inhibitors phenylpyridazine analogues (I). Both 1 and 2 were tested on the human ACAT-1 and ACAT-2 isoforms. The amino derivatives 2 were found to be inactive, contrary to the related pyridazine derivatives. By contrast, the ortho-substituted amides 1a and 1d showed an interesting activity. These results support the essential role of the pyridazine nucleus. Modeling studies were also performed.
FeCl2-Promoted Cleavage of the Unactivated CC Bond of Alkylarenes and Polystyrene: Direct Synthesis of Arylamines
作者:Chong Qin、Tao Shen、Conghui Tang、Ning Jiao
DOI:10.1002/anie.201202464
日期:2012.7.9
efficient and convenient nitrogenation strategy involving CCbondcleavage for the straightforward synthesis of versatile arylamines is presented. Various alkyl azides and alkylarenes, including the common industrial by‐product cumene, react using this protocol. Moreover, this method provides a potential strategy for the degradation of polystyrene.
In contrast to the recent breakthrough in electrochemical C–H aminations, the electrochemicallyoxidative C–N bondformation through a C–C bond cleavage is rarely studied. This work describes an electrochemical C–C amination of alkylarenes for the efficient synthesis of versatile anilines, as well as carbonyl compounds. With the cheap and durable graphite plates as electrodes, and in a simple undivided
Neue Verbindungen der Formel I worin R?1, R2, R2', R2'', R3, R4, R5, R5', R5'', R5''', R5''''¿, X, Y, U, V und W die in Patentanspruch 1 angegebene Bedeutung haben, sind Inhibitoren des Koagulationsfaktors Xa und VIIa und können zu Behandlung von Thrombosen, myocardialem Infarkt, Arteriosklerose, Entzündunden, Apoplexie, Angina pectoris, Restenose nach Angioplstie, Claudicatio intermittens, Tumoren, Tumorerkrankungen und/oder Tumormetastasen eingesetzt werden.