Ciba Specialty Chemicals Corporation

Richard Lewis Riggs

Nicholas James Westwood

Colin Morton

David Macdonald Smith

The present invention relates to a process for the preparation of furopyrroles of general formula (I), comprising (a) heating a compound of the formula (II) under microwave irradiation optionally in the presence of an inert solvent, wherein Aand Aare C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, CCcycloalkenyl, aryl or heteroaryl, Ais hydrogen, C-Calkyl, cyanomethyl, Ar, &#x2014;CRR&#x2014;(CH)&#x2014;Aror Y&#x2014;R, wherein Rand Rindependently of each other stand for hydrogen or C-Calkyl, or phenyl which can be substitute up to three times with C-Calkyl, Arstands for aryl, C-Ccloalkyl, C-Ccycloalkenyl or heteroaryl, which can be substituted one to three times with C-Calkyl, C-Calkoxy, halogen or phenyl, which can be substituted with C-Calkyl or C-Calkoxy one to three times, and m stands for 0, 1, 2, 3 or 4, R is C-Calkyl, in particular C-Calkyl, aryl, in particular phenyl, or aralkyl, in particular benzyl, which can be substituted one to three times with C-Calkyl, C-Calkoxy, or halogen, Y is &#x2014;C(O)&#x2014;, &#x2014;C(O)O&#x2014;, &#x2014;C(O)NH&#x2014;, &#x2014;SONH&#x2014; or &#x2014;SO&#x2014; and Ris C-Calkyl, Ar, or aralkyl. The furopyrroles of the general formula (I) can be can be obtained in high yield and high purity by the process of the present invention. 

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Edinburgh, United Kingdom

Richard Lewis Riggs