US 11,939,342 B2
Process for the preparation of midostaurin with high purity
Alberto Lena, Cameri (IT); Antonio Toppino, Cameri (IT); Katia Miele, Settala (IT); Jacopo Roletto, Cameri (IT); and Paolo Paissoni, Cameri (IT)
Assigned to PROCOS S.P.A., Cameri (IT)
Appl. No. 17/426,356
Filed by PROCOS S.P.A., Cameri (IT)
PCT Filed Mar. 25, 2020, PCT No. PCT/EP2020/058273
§ 371(c)(1), (2) Date Jul. 28, 2021,
PCT Pub. No. WO2020/200945, PCT Pub. Date Oct. 8, 2020.
Claims priority of application No. 102019000004729 (IT), filed on Mar. 29, 2019.
Prior Publication US 2022/0098216 A1, Mar. 31, 2022
Int. Cl. C07D 498/22 (2006.01)
CPC C07D 498/22 (2013.01) 17 Claims
 
1. A process for the preparation of midostaurin with high purity, that is with a content of 3-hydroxymidostaurin impurities (III) and (IV) lower than 0.1%, comprising treating crude midostaurin with strong organic or inorganic acids in a water-immiscible solvent and, optionally, also with reducing silanes.