| abstract |
The invention discloses a method for preparing Pacritinib (I). Through formula II compound 1-[3-(4-bromo-2-butene)methanol phenyl]-3-dimethylamino-2-propen-1-ketone and formula III compound 2-halogen-5-guanidino Phenylcarbinol is subjected to a cyclization reaction under the action of a base accelerator to obtain (16E)-11-halogen-14,19-dioxa-5,7,26-triazatetracyclo[19.3.1.1(2,6 ), 1 (8, 12)] Heptacane-1 (25), 2 (26), 3, 5, 8, 10, 12 (27), 16, 21, 23-decene (IV), intermediate The etherification reaction between body (IV) and 2-(1-pyrrolidinyl)ethanol in the presence of an acid-binding agent yields pacotinib (I). The method has the characteristics of easy-to-obtain raw materials, simple process, economy and environmental protection, and is suitable for industrialized production. The invention also discloses two intermediates that can be used for preparing pacotinib and the preparation method thereof. |