Solid phase chemistry approach to the SAR development of a novel class of active site-directed thrombin inhibitors

A solid phase chemistry approach utilizing Mitsunobu chemistry, amine functionalization, and parallel purification was used to produce a diverse library of benzothiophene analogs. These analogs were used to advance the SAR of this class of molecules and give new directions for future studies. A soli...

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Bibliographic Details
Published inTetrahedron Vol. 55; no. 39; pp. 11641 - 11652
Main Authors Johnson, Mary George, Bronson, Duane D., Gillespie, Jan E., Gifford-Moore, Donetta S., Kalter, Kyomi, Lynch, Michael P., McCowan, Jefferson R., Redick, Catherine C., Sall, Daniel J., Smith, Gerald F., Foglesong, Robert J.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier Ltd 24.09.1999
Elsevier
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
REAGENT
MITSUNOBU REACTION
POTENT
DESIGN
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Summary:A solid phase chemistry approach utilizing Mitsunobu chemistry, amine functionalization, and parallel purification was used to produce a diverse library of benzothiophene analogs. These analogs were used to advance the SAR of this class of molecules and give new directions for future studies. A solid-phase Mitsunobu reaction was utilized together with a very mild cleavage strategy to rapidly advance the SAR of a novel series of Thrombin inhibitors. Over three hundred analogs were prepared
ISSN:0040-4020
1464-5416
DOI:10.1016/S0040-4020(99)00684-5