906673-48-1Relevant articles and documents
Preparation method of crisaborole
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Paragraph 0046; 0051-0053; 0066; 0069, (2021/05/29)
The invention discloses a preparation method of crisaborole, which comprises the following steps: S1, reacting 2-bromo-5-hydroxybenzaldehyde with a hydroxyl protecting reagent in a solvent in the presence of alkali to obtain a compound I; S2, reducing the compound I in a solvent in the presence of a reducing agent to obtain a compound I I; S3, reacting the compound I with a hydroxyl protection reagent in a solvent in the presence of alkali to obtain a compound IV; S4, reacting the compound IV with boric acid ester in a solvent in the presence of alkali to obtain a compound V; S5, removing a hydroxyl protecting group from the compound V to obtain a compound VI; and S6, reacting the compound IV with p-fluorobenzonitrile to obtain crisaborole. A hydroxyl protecting group which is more beneficial to removal is adopted in the route, synthesis of boric acid ester is facilitated, side reactions are reduced, the yield is obviously increased, and the method is easy to operate, low in cost and beneficial to industrial production.
BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS
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Page/Page column 40, (2008/06/13)
Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed.
Boron-containing small molecules
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Page/Page column 26, (2008/06/13)
This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate.