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(2R*, 3S*)-1-[125I] Iodo-2, 3-bis (4-hydroxyphenyl) pentane ([125I] iodonorhexestrol), and (2R*, 3S*)-1-[77Br] bromo-2, 3-bis (4-hydroxyphenyl) pentane ([77Br] …

SW Landvatter, JA Katzenellenbogen…

文献索引:Landvatter, Scott W.; Katzenellenbogen, John A. Journal of Medicinal Chemistry, 1982 , vol. 25, # 11 p. 1300 - 1307

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被引用次数: 23

摘要

Results Chemical Synthesis. The precursor for both the 1-bromo-and 1-iodonorhexestrols (5 and 6) is the bis (ethoxyethyl ether) protected norhexestrol trifluoromethanesulfonate (triflate) 4. The alcohol (3) used in the preparation of this triflate is obtained from the norhexestrol acid methyl ester (1) 13 by reaction with ethyl vinyl ether, followed by reduction with lithium aluminum hydride (Scheme I). The inclusion of sodium methoxide in the latter ...