Synthesis of Biologically Interesting Molecules

The future direction of the field of asymmetric multicatalysed tandem reactions is to continue expanding their scope through the employment of novel combinations of (novel) catalysts which will allow novel enantioselective transformations to be discovered. These novel unprecedented one-pot reactions are expected to be rapidly applied to the synthesis of biologically interesting molecules including natural products. 

He is an author of more than 150 papers published in international scientific journals. His scientific interests cover the synthesis of biologically active molecules and the development of new methodologies directed to synthesis automation applied to drug discovery and drug optimization. 

Without doubt, multicomponent reactions have become an attractive tool for the synthesis of biologically active molecules. In this regard, Jeong et al. reported an interesting domino synthesis of bicyclopentenones [50]. They employed a bimetallic system consisting of [Pd2(dba)3(CHCl3)] and... 

The ketene dithioacetal method group has proved useful for the synthesis of a number of biologically interesting molecules <2000BML703, 2004EJM969>, including 5-cyanopyrimidine derivatives which are orally active inhibitors... 

When the approach of chiral auxiliary is used to generate a chiral center in a molecule, enzymatic resolution has become a frequently used methodology for the synthesis of biologically interesting materials with high optically active forms. 

In the synthesis of biologically important molecules, the replacement of halogen by hydrogen in four-26,48-51, five-27,52 and six-membered32,38,40,53-61 rings has seen much interest. 

Selective alkylation of 1,2,4-triazole in position 1 is of primary interest for the synthesis of biologically active molecules such as fungicides (fluconazole, flutriafole,... 

Development of new methods in organic synthesis and their applications to the synthesis of biologically interesting natural products 12CPB1. Dienamine catalysis as an emerging technology in the synthesis of bioactive molecules and natural products 12EJ0865. 

It is worth noting that the Shibasaki group also developed a highly useful protocol for asymmetric Mannich-tyip reactions (556), which was used successfully in the synthesis of biologically active molecules like nemonapride, an antipsychotic agent developed by Yamanouchi Pharmaceutical. Since such a useful application of this methodology is not a bom fide natural product synthesis, a detailed discussion is beyond the scope of this contribution and the interested reader is referred to Shibasaki s original report (556). 

Part Three is intended to balance the coverage of Parts One and Two and to serve as a convenient guide to the now enormous literature of multistep synthesis. Information on more than five hundred interesting multistep syntheses of biologically derived molecules is included. It is hoped that the structural range and variety of target molecules presented in Part Three will appeal to many chemists. 

The stereoselective synthesis of carbohydrates from acyclic precursors is a research topic that has attracted considerable attention over the past decadeT Efforts in this area are easily justified and have maximum impact particularly when directed toward rare sugars or other polyhydroxylated molecules that are not conveniently accessed via classical "chiron" approaches.2 An underlying theme of such efforts, of course, is the development of practical synthetic methodology that will find broad application in the enantio- and diastereoselective synthesis of natural products, their analogues, and other compounds of biological interest. 

Occurrence in nature of branched-chain carbohydrates has prompted interest in the syntheses of these complex structures and stimulated the preparation of analogues for biological evaluation. Consequently, new methods for the construction of these particular skeletons have been devised [1]. The use of carbohydrates as a cheap source of chiral starting materials [2-4] for the synthesis of complex, nonsugar molecules has prompted the emergence of new imaginative methods for formation of carbon-carbon bonds adapted to the particular reactivity of sugar moieties. 

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