CPC C07F 5/025 (2013.01) [C07C 253/30 (2013.01); C07C 255/54 (2013.01)] | 4 Claims |
1. A process for preparation of crisaborole of a compound of formula (I) through use of a compound of formula (IV), (III) or (II), comprising:
reacting the compound of formula (IV) with a borylation reagent to provide the compound of formula (III);
optionally transesterifying the compound of formula (III) with diethanolamine in suitable solvent to provide the compound of formula (II);
deprotecting and cyclizing the compound of formula (II) or (III) for the preparation of crisaborole of formula (I); and
wherein the compound of formula (IV) is,
where X=Cl, Br, I, F or Triflate,
wherein the compound of formula (III) is,
wherein the compound of formula (II) is,
wherein the compound of formula (I) is,
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