CAS: 145821-59-6; (R)-1-(4,4-Bis(3-Methylthiophen-2-yl)But-3-En-1-yl)Piperidine-3-Carboxylic Acid Hydrochloride

📜氢溴酸槟榔碱置于盐酸,C63H78Irnop(2+)*c32H12Bf24(1-),水,氢气,Potassium Carbonate,Potassium Iodide,Sodium Hydroxide体系中,用 甲醇,二氯甲烷,水,丙酮 用作溶剂,20.0~60.0 °C,607.99 Kpa 条件下,反应 135.5H,反应生成盐酸噻加宾
参考文献:铱催化不饱和杂环酸的对映选择性加氢
标题:铱催化不饱和杂环酸的对映选择性加氢
摘要:螺旋结合:一种高度对映选择性的不饱和杂环羧酸的加氢已经通过使用手性铱/ Spirophosphino恶唑啉催化剂开发(参见方案; Bar ˚f-=四[3,5-双(三氟甲基)苯基]硼酸盐,的boc =叔丁氧羰基) .该反应提供了制备具有优异对映选择性的旋光杂环酸的有效方法.
Doi:10.1002/anie.201301341

专利信息

专利号:US-2011040105-A1
优先权日:2008-04-16
标题 :Processes useful for the synthesis of (r)-1--2-methyl-pyrrolidine
发明人：HUBER CHRISTIAN H; KHULMAN YOUNG MI; TANDEL SAGUN K; JOHANNSEN STEPHEN R; WANG TINGMIN; ANGELL PAUL
权利人:ARENA PHARM INC
摘要:Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.

专利号:US-12201669-B2
优先权日:2021-03-11
标 题:Small molecule suppressors of APOE gene expression and cerebral vascular amyloid pathology
发明人：TSAI LI-HUEI; BLANCHARD JOEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using small molecule inhibitors. The invention also includes methods of treating disease associated with amyloid synthesis, such as Alzheimer's disease. The small molecule inhibitors disclosed herein are compounds which are non-immunosuppressant cyclosporin including the pharmaceutically acceptable salts thereof.

专利号:CN-102066319-A
优先权日:2008-04-16
标 题 :Processes useful for the synthesis of (R)-1-{2-[4'-(3-methoxypropane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine

专利号:EP-2282992-A1
优先权日:2008-04-16
标 题 :Processes useful for the synthesis of (r)-1-{2-ý4'-(3-methoxypropane-1-sulfonyl)-biphenyl-4-yl¨-ethyl}-2-methyl-pyrrolidine

专利号:WO-2009128907-A1
优先权日:2008-04-16
标 题 :Processes useful for the synthesis of (r)-1-{2-[4'-(3-methoxypropane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine

专利号:US-12285440-B2
优先权日:2021-03-14
标题 :APOE4 impairs myelination via altered cholesterol biosynthesis and transport in oligodendroglia
发明人：BLANCHARD JOEL; KELLIS MANOLIS; TSAI LI-HUEI; DAVILA VELDERRAIN JOSE; AKAY LEYLA; VON MAYDELL DJUNA; EFFENBERGER AUDREY; VICTOR MATHEUS
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides methods of inhibiting amyloid synthesis in a subject using cyclodextrin and analogs thereof. Small molecules (cyclodextrin) reverse APOE4-associated cholesterol phenotypes and lead to significantly improved myelination both human in vitro cultures and APOE4 targeted replacement mice. This demonstrates that APOE4 alters cholesterol synthesis and transport in oligodendrocytes which impairs myelination. Collectively, this work uncovers a pathogenic role of APOE4 in oligodendrocytes and myelination and enables therapeutic opportunities for Alzheimer's Disease.