Crisaborole (code AN-2728) a non-steroidal boron containing drug is a phosphodiesterase-4 inhibitor, used for topical treatment of psoriasis and atopic dermatitis

摘要

Crisaborole (code AN-2728) a non-steroidal boron containing drug is a phosphodiesterase-4 inhibitor, used for topical treatment of psoriasis and atopic dermatitis. The chemical name of crisaborole is 5-(4-cyanophenoxy)-l-hydroxy-l,3-dihydro-2.1-bena)xaborole and has following structure: US8039451B2 discloses Crisaborole and pharmaceutical formulation containing it. US '451 also discloses process for preparation of Crisaborole in example-4. The process disclosed in the patent suffers from several disadvantages, as it utilizes of flash column chromatography to purify the product it is a cumbersome, expensive and time consuming technique. Further the product is obtained in very low yield and has only 80% purityeven after column purification. Hence, one or more purification steps are required to purify the obtained compound in order to comply with various regulatory requirements.