Short-step synthesis of tamoxifen and its derivatives via the three-component coupling reaction and migration of the double bond |
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| Authors: | Isamu Shiina Masahiko Suzuki Kazutoshi Yokoyama |
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| Institution: | Department of Applied Chemistry, Faculty of Science, Tokyo University of Science, Kagurazaka, Shinjuku-ku, Tokyo 162-8601, Japan |
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| Abstract: | The anti-tumor agent, tamoxifen, is easily synthesized by the successive allylation of benzaldehyde and the Friedel-Crafts alkylation reaction of anisole with the intermediary homoallyl silyl ethers, followed by the migration of the double bond to form the desired tetra-substituted ethylenes. Several derivatives of tamoxifen are also produced according to a similar synthetic strategy. |
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