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Oxetanes as Versatile Elements in Drug Discovery and Synthesis
Author(s) -
Burkhard Johannes A.,
Wuitschik Georg,
RogersEvans Mark,
Müller Klaus,
Carreira Erick M.
Publication year - 2010
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200907155
Subject(s) - oxetane , stereocenter , computer science , drug discovery , biochemical engineering , nanotechnology , computational biology , combinatorial chemistry , chemistry , materials science , biology , engineering , organic chemistry , biochemistry , enantioselective synthesis , catalysis
Sizable resources, both financial and human, are invested each year in the development of new pharmaceutical agents. However, despite improved techniques, the new compounds often encounter difficulties in satisfying and overcoming the numerous physicochemical and many pharmacological constraints and hurdles. Oxetanes have been shown to improve key properties when grafted onto molecular scaffolds. Of particular interest are oxetanes that are substituted only in the 3‐position, since such units remain achiral and their introduction into a molecular scaffold does not create a new stereocenter. This Minireview gives an overview of the recent advances made in the preparation and use of 3‐substituted oxetanes. It also includes a discussion of the site‐dependent modifications of various physicochemical and biochemical properties that result from the incorporation of the oxetane unit in molecular architectures.