Effective synthesis of tamoxifen using nickel-catalyzed arylative carboxylation

被引：41

作者：

Shimizu, Kazuya

Takimoto, Masanori

Mori, Miwako ^{[1
]}

Sato, Yoshihiro

机构：

[1] Hokkaido Univ, Grad Sch Pharmaceut Sci, Sapporo, Hokkaido 0600812, Japan

[2] RIKEN, Inst Phys & Chem Res, Organomet Chem Lab, Wako, Saitama 3510198, Japan

[3] Hlth Sci Univ Hokkaido, Ishikari, Hokkaido 0610293, Japan

来源：

SYNLETT | 2006年 / 18期

关键词：

tetrasubstituted alkenes; nickel catalyst; zinc reagent; tamoxifen; carbon dioxide;

D O I：

10.1055/s-2006-951517

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Tamoxifen was synthesized using a nickel-catalyzed arylative carboxylation developed by our group. The key compound, tetrasubstituted alkene, was synthesized from disubstituted alkyne using a catalytic amount of Ni(0) and DBU in the presence of Ph2Zn under an atmosphere of carbon dioxide. The reaction proceeded smoothly in a regio- and stereoselective manner, and the resultant tetrasubstituted alkene was converted into tamoxifen.

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页码：3182 / 3184

页数：3

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