CAS: 159752-10-0; (R)-2-Amino-N-(3-(Benzyloxy)-1-(1-(Methylsulfonyl)Spiro[indoline-3,4'-Piperidin]-1'-yl)-1-Oxopropan-2-yl)-2-Methylpropanamide Methanesulfonate

上下游产品

isonipecotic acid N-B°C-D-serine(Bzl)-OH benzyl bromide 1-benzyloxycarbonylpiperidine-4-carboxylic acid

螺[吲哚啉-3,4'-哌啶]-1'-羧酸苄酯置于palladium On Activated Charcoal 甲烷磺酸,氢气,1-羟基苯并三唑,N,N-二异丙基乙胺,N,N'-二环己基碳二亚胺体系中,用 四氢呋喃,乙醇,水,乙酸乙酯 用作溶剂,5.0~65.0 °C,275.79 Kpa 条件下,反应 21.5H,反应生成伊布莫仑甲磺酸盐
参考文献:合成基于口服螺螺吲哚的生长激素促分泌素mk-677
标题:合成基于口服螺螺吲哚的生长激素促分泌素mk-677
摘要:默克生长激素促分泌素的制备;描述了mk-677.费歇尔吲哚/还原为基础的策略提供了这种有效化合物的新型螺二氢吲哚核.该优化的序列仅需要分离一种中间体10并从异二十二烯酸3提供48%的总收率的mk-677 .
Doi:10.1016/s0040-4020(97)00359-1

专利信息

专利号:US-9751877-B2
优先权日:2012-09-21
标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-9771379-B2
优先权日:2015-09-24
标题:N-(2-(2-amino-6-substituted-4,4a,5,6-tetrahydropyrano[3,4-d][1,3]OXAZIN-8a(8H)-yl)-thiazol-4-yl) amides
发明人：BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; ZHANG LEI; O'NEILL BRIAN THOMAS
权利人:PFIZER
摘要:The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, n nwherein the variables R 1 , R 2 , R 3 , R 4 and X are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:WO-2012172449-A1
优先权日:2011-06-13
标题:Lactams as beta secretase inhibitors
发明人：BRODNEY MICHAEL AARON
权利人:PFIZER; BRODNEY MICHAEL AARON
摘要:Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compound of formula I is useful as beta secretase inhibitor for use in the treatment of Alzheimer's and other neurodegenerative and/or neurological disorders.

专利号:US-2016229847-A1
优先权日:2013-10-04
标 题:Novel bicyclic pyridinones as gamma-secretase modulators
发明人：PETTERSSON MARTIN YOUNGJIN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; JOHNSON DOUGLAS SCOTT; KAUFFMAN GREGORY WAYNE; O'DONNELL CHRISTOPHER WILLIAM; PATEL NANDINI CHATURBHAI; STEPAN ANTONIA FRIEDERIKE; STIFF CORY MICHAEL; SUBRAMANYAM CHAKRAPANI; TRAN TUAN PHONG; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula II as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-9067934-B2
优先权日:2011-03-31
标题 :Bicyclic pyridinones
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; FISH BENJAMIN ADAM; GREEN MICHAEL ERIC; MULLINS PATRICK BRADLEY; STIFF CORY MICHAEL; TRAN TUAN PHONG; NAVARATNAM THAYALAN
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:US-8962616-B2
优先权日:2012-05-04
标 题:Heterocyclic substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
发明人：BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; BECK ELIZABETH MARY; DAVOREN JENNIFER ELIZABETH; O'NEILL BRIAN THOMAS
权利人:PFIZER
摘要:Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.