| 摘要 |
<p>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, process which consists in protecting the 1-position in question with a labile protecting group, reacting the compound so obtained with a lithiation agent selected from a lithium amide and an alkyl lithium at a temperature between -80 DEG C. and -20 DEG 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 DEG C. and room-temperature with a reagent capable of giving rise to an electrophilic group to form N-protected 1H-pyrrolo[3,2-c]pyridine substituted in the 2-position by an electrophilic group.</p> |
