Title of article
A practical synthesis of LFA-1 inhibitors utilizing CuCl-promoted intramolecular cyclization of thiohydantoins
Author/Authors
Wang، نويسنده , , Xiaojun and Zhang، نويسنده , , Li and Xu، نويسنده , , Yibo and Krishnamurthy، نويسنده , , Dhileepkumar and Varsolona، نويسنده , , Richard and Nummy، نويسنده , , Laurence and Shen، نويسنده , , Sherry and Frutos، نويسنده , , Rogelio P. and Byrne، نويسنده , , Denis and Chung، نويسنده , , J.C. and Farina، نويسنده , , Vittorio and Senanayake، نويسنده , , Chris H.، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2005
Pages
4
From page
273
To page
276
Abstract
An efficient and chromatography-free approach for synthesis of a new class of LFA-1 inhibitors was developed. A copper(I) chloride-promoted intramolecular cyclization of thiohydantoins 7a–b serves as a key step to highly functionalized bicyclic guanidines 5a–b, that were subsequently converted to 1H-imidazo[1,2-a]imidazol-2-one LFA-1 inhibitors. This process has been successfully implemented in the pilot plant to produce multikilogram quantities of LFA-1 inhibitors such as 1a–b.
Keywords
imidazolidinone , Bicyclic guanidine , LFA-1 inhibitor , Thiohydantoin
Journal title
Tetrahedron Letters
Serial Year
2005
Journal title
Tetrahedron Letters
Record number
1844420
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