Phthalimide analogues have been extensively used in medicinal chemistry owing to their wide range of applications as anti-convulsant, anti-inflammatory, analgesic, hypolipidimic and immunomodulatory activities. Number of anti-inflammatory phthalimide analogues have been synthesized as tumor necrosis factor-α (TNF-α) inhibitors. TNF-α plays a critical role in certain physiological immune systems and its over-production causes severe damage to the host. It promotes the inflammatory response leading to many of the clinical problems associated with auto-immune disorders like rheumatoid arthritis, Crohns disease, ankylosing spondylitis, psoriasis and refractory asthma. One of the phthalimide derivatives, LASSBio-468, was recently demonstrated to inhibit TNF-α production induced by lipopolysaccharide (LPS), in vivo. Its potential against chronic inflammatory diseases was also witnessed. Another derivative, DIMP, showed good anti-androgenic activity. These analogues have also been employed for the synthesis of several kinds of important therapeutic synthones. However extensive research on the chemistry and biological activities of phthalimide analogues has been carried out and number of reports appeared, a compilation focusing on chemistry and biological activity is still needed. This review, concisely describes the chemical and therapeutic aspects of phthalimide derivatives.
Silylation of hydrocarbons is one of the most important transformations due to the diverse application of organosilanes. Continuous progress is being made in organosilane synthesis particularly through direct C–H activation/functionalization. This minireview compiles various processes reported for C–Si bond formation from 2000–2014, through C–H activation/functionalization (proximal and remote) and metal-free approaches. 1 Introduction 2 C–Si Bond Formation through C–H Activation in Intermolecular Fashion 2.1 C–Si Bond Formation through Direct C(sp2)–H Activation 2.2 C–Si Bond Formation through Directing Group Assisted C(sp2)–H Activation 2.3 C–Si Bond Formation through sp3 C–H Activation 3 C–Si Bond Formation through Proximal C–H Activation/Functionalization in Intramolecular Fashion 3.1 Intramolecular C–Si Bond Formation through C(sp2)–H Activation 3.2 Intramolecular C–Si Bond Formation through C(sp3)–H Activation 4 Siloles Synthesis through Heteroannulation 5 C–Si Bond Formation through Remote C–H Activation 6 C–Si Bond Formation through C–O Bond Cleavage 7 Metal-Free Methods for C–Si Bond Formation 8 Summary and Outlook
21 June 2013 in European Journal of Organic Chemistry