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ABSTRACT:
Synthon approach advocated by Prof. E. J. Corey of Harvard University has emerged as a powerful analytical tool of design synthetic routes for the preparation of an organic compound of any interest from readily available starting materials. This approach plays a vital role in the synthesis of medicinal compounds/drugs which is a part and parcel of modern drug discovery process. Taking the privilege of this approach, a good number of synthesis schemes has been proposed for a potent anti-diabetic agent "rosiglitazone" keeping an overview on the works published in both journals and patent literatures. The proposed synthesis planning being a theoretical investigation, the actual laboratory execution requires the cross examination of a considerable number of factors such as reactions, reagents and order of events. In actual practice, generally that route is most feasible which is cost-effective, safe, and easy to carry out and produces maximum yield in a short reaction time.
KEYWORDS: Anti-diabetic agent, Drug synthesis, Synthon approach, Retrosynthetic analysis, Rosiglitazone.
1. INTRODUCTION
The heart of organic synthesis is designing synthetic routes to a molecule. The simplest synthesis of a molecule is one in which the target molecule can be obtained by submitting a readily available starting material to a single reaction that converts it to the desired target molecule. However, in most cases the synthesis is not that straightforward; in order to convert a chosen starting material to the target molecule, numerous steps that add, change, or remove functional groups and steps that build up the carbon atom framework of the target molecule may need to be done. A systematic approach for designing synthetic routes to a molecule is promulgated as a result of Prof. E.J. Corey's developments of synthon disconnection approach/retrosynthetic analysis.1,2,3 Retrosynthetic analysis is a protocol of stepwise breaking of target molecule to starting materials by disconnection of bonds and functional group interchange to a sequence of progressively simpler structures along a pathways just reverse of actual synthesis. Every disconnected part is an idealized fragment, called 'synthon.'
The synthons when joined by known or conceivable synthetic operations result in the formation of target molecule. Retrosynthetic analysis of a target molecule usually results in more than one possible synthetic route. It is therefore necessary to critically assess each derived route...