351418-50-3Relevant articles and documents
Preparation method of crisaborole
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Paragraph 0046-0050; 0066-0068, (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.
Synthesis of Monodisperse Naphthalene Dendrons for the Application of Dendrimers
Jillella, Raveendra,Kim, Jaewoong,Kim, Kun Hee,Han, Jin Wook,Oh, Chang Ho
supporting information, p. 1090 - 1095 (2018/09/06)
Syntheses of dendrons for dendrimer applications are described using napthyl and urethane derivatives. The napthol, 1-(3-hydroxy-6-(methoxymethoxy)naphthalen-1-yl)ethan-1-one (h), was synthesized by employing Au-catalyzed cyclization of the corresponding
1H-phosphindoles as structural units in the synthesis of chiral helicenes
Yavari, Keihann,Moussa, Souad,Ben Hassine, Béchir,Retailleau, Pascal,Voituriez, Arnaud,Marinetti, Angela
supporting information; experimental part, p. 6748 - 6752 (2012/08/28)
Building helicenes: A photochemical cyclization approach affords helicenes in which the fused ring sequence ends with a phosphole unit (see scheme). The stereogenic phosphorus centers of the substrates control the screw sense of helical chirality. The terminal phosphole units undergo photochemical [2+2] annulations to give dimeric helical structures. Copyright