Simple preparations of 4 and 5-iodinated pyrazoles as useful building blocks

Tetrahedron 2011, 67, 8451-8457

The pyrazole nucleus has recently become a recurrent scaffold in the research fields of CropScience and oncology. We report here the preparation of an array of 4- and 5-iodinated pyrazole derivatives, such as 4-iodo-3-trifluoromethylpyrazole or ethyl 5-iodo-4-carboxy-3-trifluoromethylpyrazoles. This work provide access to many new pyrazole derivative, including 11 original out of 16 iodinated building blocks, thus opening accesses to new chemical entities featuring a pyrazole nucleus