- A new Suzuki synthesis of triphenylethylenes that inhibit aromatase and bind to estrogen receptors α and β
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The design and synthesis of dual aromatase inhibitors/selective estrogen receptor modulators (AI/SERMs) is an attractive strategy for the discovery of new breast cancer therapeutic agents. Previous efforts led to the preparation of norendoxifen (4) deriva
- Zhao, Li-Ming,Jin, Hai-Shan,Liu, Jinzhong,Skaar, Todd C.,Ipe, Joseph,Lv, Wei,Flockhart, David A.,Cushman, Mark
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p. 5400 - 5409
(2016/10/24)
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- Olefination of aromatic ketones: Synthesis of mono- and dihaloalkenes
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A new simple and efficient transformation of various aromatic ketones to the corresponding halo (dihalo) alkenes is described. The reaction proceeds under mild conditions to give the target products in good yields.
- Korotchenko, Vasily N.,Shastin, Alexey V.,Nenajdenko, Valentine G.,Balenkova, Elisabeth S.
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p. 883 - 887
(2007/10/03)
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- Preparation of 1-bromo-1-chloro-,1,1-dibromo- or 1,1-dichloroalk-1-enes from ketones
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An efficient three steps process for converting aliphatic ketones to the homologous gem-bromochloro, or gem-dibromo alkenes is presented.
- Rezaei, Hadi,Normant, Jean F.
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p. 109 - 112
(2007/10/03)
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- Reactions of 1,1-Dihaloalkenes with Triorganozincates: A Novel Method for the Preparation of Alkenylzinc Species Associated with Carbon-Carbon Bond Formation
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Lithium trialkylzincates react with 1,1-dibromoalkenes 1 and 1-bromo-1-chloroalkenes 2 at -85 deg C in THF to give 1-bromoalkenes 5 and 1-chloroalkenes 7, respectively, upon hydrolysis.The intermediate (1-haloalkenyl)zincates 4 and 6 are stable at low temperature but, when allowed to warm to 0 deg C, they undergo a 1,2-alkyl migration reaction to afford alkenylzinc species 10.A variety of alkylation products 11 are obtained by the hydrolysis of 10.In the presence of (Ph3P)2Pd (5 molpercent), alkenylzinc species 10 react smoothly with organic halides (AcCl, EtOCOCl, CH2=CH(Me)Br, PhBr) to yield the corresponding coupling products 13-16.
- Harada, Toshiro,Katsuhira, Takeshi,Hara, Daiji,Kotani, Yasuo,Maejima, Keiji,et al.
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p. 4897 - 4907
(2007/10/02)
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