Process for the preparation of 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol and (R)-feso-deacyl
    8.
    发明授权
    Process for the preparation of 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol and (R)-feso-deacyl 有权
    制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇和(R) - 壬酰基

    公开(公告)号:US08946456B2

    公开(公告)日:2015-02-03

    申请号:US13702403

    申请日:2011-04-29

    摘要: The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.

    摘要翻译: 本发明涉及一种改进的和工业上有利的制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇中间体的方法,也称为“feso chromenyl”和(R) -2- [3-(二异丙基氨基)-1-苯基丙基] -4-(羟甲基)苯酚,也称为“(R) - 非索酰基”,它们又用于合成西索罗定,特别是富马酸非索罗定。 该方法利用在工业水平上无毒且易于管理的试剂,能够获得称为B型关键中间体“(R) - feso deacyl”的新型稳定和非吸湿结晶形式。