我们报告了通过初始ICl促进的双(Biaryl)乙炔的初始ICl环化,然后进行Mizoroki-Heck偶联反应,轻松合成功能化的二苯并[ g,p ]。该新方法对于各种双(联芳基)乙炔很好地起作用,以提供具有各种官能度的二苯并[ g ] ,[ p ]。对于包括4'-甲氧基-2-乙炔基联苯在内的一种特殊类型的底物,我们发现ICl处理导致ipso环化生成双环螺环己二酮。在MeOH / H 2 SO 4的存在下,这些螺酮产品经过选择性的1,2-链烯基迁移而发生重排,从而生成9-碘菲。我们制备了各种4'-甲氧基-2-乙炔基联苯化合物,以显示这种ipso环化和1,2-烯基转移的一般性。此本位-cyclization方法可以扩展二苯并[的制备克,p ] chrysenes。
PHARMACEUTICAL FORMULATIONS FOR USE IN ESTROGEN DEPRIVATION SYNDROME
申请人:ELI LILLY AND COMPANY
公开号:EP1121125A1
公开(公告)日:2001-08-08
BENZOTHIOPHENE DERIVATIVES AND COMPOSITIONS THEREOF AS SELECTIVE ESTROGEN RECEPTOR DEGRADERS
申请人:Novartis AG
公开号:EP2958907B1
公开(公告)日:2018-02-28
[EN] PHARMACEUTICAL FORMULATIONS FOR USE IN ESTROGEN DEPRIVATION SYNDROME<br/>[FR] FORMULATIONS PHARMACEUTIQUES DE TRAITEMENT DU SYNDROME DE CARENCE OESTROGENIQUE
申请人:LILLY CO ELI
公开号:WO2000021535A1
公开(公告)日:2000-04-20
Formulations and applications thereof are described which are useful for the inhibition of various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of structure (I) in combination with compounds of formula (II) where X, Y, R, R', R?6, R7, and R8¿ are as defined herein.