专利号:US-6448419-B1 优先权日:2001-08-07 标题:Synthesis of 2-hydroxyestradiol derivatives 发明人:PAAREN HERBERT E; DUFF STEVEN R 权利人:TETRIONICS INC 摘要:Disclosed is a method of preparing 2-hydroxy-3,17β-estradiol derivatives wherein 3,17β-estradiol is reacted with an organolithium reagent and reacted with either a boron reagent or a silicon reagent to form either a 2-boronyl or a 2-silyl modified estradiol analog represented by the corresponding structural formulae: n R 1 and R 2 are each independently a hydroxyl protecting group. R 3 , R 4 and R 5 are selected from the group consisting of halogens, alkyl, aryl, hydroxy, substituted or unsubstituted alkyl, and substituted or unsubstituted aryl.
专利号:US-6054598-A 优先权日:1997-03-13 标题 :Synthesis of 2-alkoxyestradiols 发明人:SACHDEVA YESH; RAM SIYA 权利人:PHARM ECO LAB INC 摘要:Disclosed is a method of preparing a compound represented by the following structural formula: The method comprises reacting bromine (Br2) and an aliphatic organic acid with a compound represented by the following structural formula: R1 and R2 are each independently a hydroxyl protecting group.
专利号:US-6051726-A 优先权日:1997-03-13 标 题 :Synthesis of 2-alkoxyestradiols
1: Wang H, Wu J. 17β-estradiol suppresses hyperoxia-induced apoptosis of oligodendrocytes through paired-immunoglobulin-like receptor B. Mol Med Rep. 2016 Jan 27. doi: 10.3892/mmr.2016.4808. [Epub ahead of print] doi: 10.1371/journal.pone.0147133. eCollection 2016. 9: Vacca V, Marinelli S, Pieroni L, Urbani A, Luvisetto S, Pavone F. 17beta-estradiol counteracts neuropathic pain: a behavioural, immunohistochemical, and proteomic investigation on sex-related differences in mice. Sci Rep. 2016 Jan 8;6:18980. doi: 10.1038/srep18980. 10: Shiga T, Nakamura TJ, Komine C, Goto Y, Mizoguchi Y, Yoshida M, Kondo Y, Kawaguchi M. A Single Neonatal Injection of Ethinyl Estradiol Impairs Passive Avoidance Learning and Reduces Expression of Estrogen Receptor α in the Hippocampus and Cortex of Adult Female Rats. PLoS One. 2016 Jan 7;11(1):e0146136. doi: 10.1371/journal.pone.0146136. eCollection 2016.
合成参考文献
摘要:Witt, D., Science of Synthesis Knowledge Updates, (2011) 3, 277. 摘要:Herter, S.; Turner, N. J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 67.