80304-50-3Relevant articles and documents
A Continuous-Flow Method for the Desulfurization of Substituted Thioimidazoles Applied to the Synthesis of Etomidate Derivatives
Baumann, Marcus,Baxendale, Ian R.
, p. 6518 - 6524 (2017/12/02)
A simple yet robust flow set-up for the efficient desulfurization of a series of thioimidazoles is presented, which generates the corresponding imidazole derivatives in high yields. The strategic choice of peristaltic over piston pumps allowed reliable delivery of the heterogeneous stream of the thioimidazole substrate into a T-piece where it reacted with NaNO2 in the presence of acetic acid. This approach enabled the controlled and safe formation of the reactive nitrosonium species without uncontrolled exposure to hazardous nitrous oxide by-products as observed in related batch protocols. The value of the resulting imidazole products was further demonstrated by their conversion into various esters representing new derivatives of the known analgesic etomidate through an efficient one-pot Corey–Gilman–Ganem oxidation procedure.
AZOLE HETEROCYCLIC COMPOUND, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE
-
, (2014/06/25)
The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.
Structure-based design of imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase
Ohkanda, Junko,Strickland, Corey L.,Blaskovich, Michelle A.,Carrico, Dora,Lockman, Jeffrey W.,Vogt, Andreas,Bucher, Cynthia J.,Sun, Jiazhi,Qian, Yimin,Knowles, David,Pusateri, Erin E.,Sebti, Said M.,Hamilton, Andrew D.
, p. 482 - 492 (2008/02/04)
A series of imidazole-containing peptidomimetic PFTase inhibitors and their co-crystal structures bound to PFTase and FPP are reported. The structures reveal that the peptidomimetics adopt a similar conformation to that of the extended CVIM tetrapeptide,