1182906-72-4Relevant articles and documents
New rafenacin intermediate, active electrophilic building block thereof and new preparation method of rafenacin
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Paragraph 0044-0050, (2021/04/26)
The invention provides a new rafenacin intermediate, an active electrophilic building block thereof and a new preparation method of rafenacin. The new rafenacin intermediate shown as the formula (II) is prepared by sequentially reacting N-methylethanolamine with a compound shown as a formula (III) and a compound shown as a formula (V), and the new rafenacin intermediate shown as the formula (II) is used for activating hydroxyl to prepare an active electrophilic block shown as a formula (VI) and then reacts with a compound shown as a formula (VII) to obtain the rafenacin shown as the formula (I). The synthetic route provided by the invention has the advantages of short reaction steps, low raw material cost, simple reaction operation, mild conditions, high conversion rate, high selectivity and convenient post-treatment, and is more suitable for industrial production.