CAS: 1643-73-8; 4-Fluorobenzylmagnesium Chloride

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CAS号352-11-4 对氟氯苄

📜4-氟氯苄置于magnesium体系中,用 四氢呋喃 用作溶剂,化学反应 2.17H,反应生成4-氟苄基氯化镁
参考文献:Strategy For The Enantioselective Synthesis Of Trans-2,4-Disubstituted Piperidines: Application To The Ccr3 Antagonist Is811
标题:Strategy For The Enantioselective Synthesis Of Trans-2,4-Disubstituted Piperidines: Application To The Ccr3 Antagonist Is811
摘要:A Strategy For The Enantioselective Synthesis Of Trans-2,4-Disubstituted Piperidines Is Proposed And Applied To The Preparation Of Is811,A Potent Ccr3 Antagonist. The C2 Stereocenter Is Derived From Commercial (R)-Epichlorohydrin,While The C4 Stereocenter Is Installed Via Diastereoselective Hydrogenation Of An Alpha,Beta-Unsaturated Lactone Intermediate. Inversion Of The Original Stereocenter Via An Efficient Intramolecular S(N)2 Amination Affords The Piperidine Core Of Is811. An Improved Protocol For The Lithiation Of Ethyl Propiolate Is Reported.
Doi:10.1021/jo0616963

专利信息

专利号:US-2003225132-A1
优先权日:2002-04-11
标题:Estrogen receptor modulators
发明人：DININNO FRANK P; HAMMOND MILTON LLOYD
摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

专利号:US-6750213-B2
优先权日:2000-10-19
标题:Estrogen receptor modulators
发明人：DININNO FRANK P; WU JANE Y; KIM SEONGKON; CHEN HELEN Y
权利人:MERCK & CO INC
摘要:The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.