1h-pyrrolo ¬3,2-c|pyridines and their preparation

Details 1h-pyrrolo ¬3,2-c|pyridines and their preparation 1h-pyrrolo ¬3,2-c|pyridines and their preparation

C - Chemistry, Metallurgy

07

D

260/273

C07D 471/04 (2006.01) C07F 7/08 (2006.01) C07F 7/10 (2006.01)

Patent

CA 1299183

ABSTRACT OF THE DISCLOSURE: The invention relates to a process for fixing an electrophilic group in the 2-position of 1H-pyrrolo[3,2-c] pyridine N-protected in the 1-position. This process consists in protecting the 1-position of the derivative with a labile protecting group, reacting the compound lo obtained with a lithiation agent selected from a lithium amide and an alkyl lithium at a temperature between -80°C and -20°C and in the presence of tetramethylethylenediamine to obtain the corresponding 2-lithio derivative and then condensing the metal derivative so obtained at a temperature between -80°C and room-temperature with a reagent capable of giving rise to an electrophilic group to form N-protected 1H- pyrrolo[3,2c]pyridine substituted in the 2-position by an electrophilic group. The derivatives that are so obtained are useful as intermediate products, particularly for the preparation of biologically active compounds, especially anthelmintic compounds.

497380

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