US2021070781A1PendingUtilityA1
A process for the preparation of crisaborole
Est. expiryDec 21, 2037(~11.4 yrs left)· nominal 20-yr term from priority
C07B 2200/13C07C 253/30C07C 255/54C07B 47/00B01J 23/42C07F 5/027C07F 5/025C07C 39/15B01J 27/053C07C 39/205B01J 23/44C07C 37/02B01J 27/232
56
PatentIndex Score
0
Cited by
0
References
0
Claims
Abstract
The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):
Claims
exact text as granted — not AI-modified1 - 15 . (canceled)
16 . A process for the purification of Crisaborole which comprises dropwise addition of a 5:1 to 8:1 acetone:water mixture of the compound to water, followed by stirring at room temperature and filtration of the resulting product.
17 . A process according to claim 1 comprising the dropwise addition of a 7:1 acetone:water mixture.
18 . A process according to claim 1 wherein crisaborole of formula (I)
is obtained by:
a) converting compound of formula (II):
into compound of formula (III):
in the presence of a tri (C 1 -C 4 ) alkyl borate and a (C 4 -C 6 )alkyl lithium or aryl lithium and subsequent acidification of the reaction medium; and
b) converting the resulting compound of formula (III) into Crisaborole of formula (I) by catalytic hydrogenation.Join the waitlist — get patent alerts
Track US2021070781A1 — get alerts on status changes and closely related new filings.
We store only your email — no account needed. See our privacy policy.