15917-60-9Relevant articles and documents
Catalytic carbometalation/cross-coupling sequence across alkynyl(2-pyridyl)silanes leading to a diversity-oriented synthesis of tamoxifen-type tetrasubstituted olefins
Kamei, Toshiyuki,Itami, Kenichiro,Yoshida, Jun-Ichi
, p. 1824 - 1835 (2007/10/03)
A general synthetic scheme for tamoxifen-type tetrasubstituted olefins based on the novel Cu-catalyzed carbomagnesation across alkynyl(2-pyridyl)silane has been developed. A wide array of electronically and structurally diverse tetrasubstituted olefins can be prepared in a regiocontrolled, stereo-controlled, and diversity-oriented manner. Noteworthy features are that (i) the three aryl groups, which are believed to be important (essential) for anti-estrogenic activity, can be varied at will because they all stem from readily available aryl iodides, and (ii) any stereo- and regioisomers can, in principle, be prepared by simply changing the order use of the aryl iodides in the sequence.