CAS: 33240-34-5; Cyclopentylmagnesium Bromide

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CAS号137-43-9 溴代环戊烷 | CAS号111848-16-9 dicyclopentyl(2... | CAS号104681-55-2 Cyclopentanecar... | CAS号111982-45-7 2-氟苯基 环戊基 酮 | CAS号3814-30-0 溴甲基环戊烷 | CAS号3400-45-1 环戊甲酸 | CAS号52829-98-8 2-环戊烷乙醇 | CAS号339549-67-6 环戊基(3-甲氧基苯基)甲酮 | CAS号3524-75-2 烯丙基环戊烷 | CAS号5422-88-8 苯基环戊基酮 | CAS号1462-06-2 Cyclopentanemet...

溴代环戊烷置于magnesium体系中,用 四氢呋喃 用作溶剂,化学反应 3.0H,反应生成环戊基溴化镁
参考文献:配体控制和无配体系统下钯催化二氯杂芳烃交叉偶联的非常规位点选择性
标题:配体控制和无配体系统下钯催化二氯杂芳烃交叉偶联的非常规位点选择性
摘要:与氮相邻的卤化物通常在二卤代n-杂芳烃的 Pd 催化交叉偶联中更具反应性.然而,空间位阻非常大的n-杂环卡宾配体被证明可以在 2,4-二氯吡啶的 C4 处以高选择性 (~10:1) 促进室温交叉偶联.这项工作代表了第一个具有广泛范围的高选择性方法,用于这些底物的 C4 偶联,其中选择性明显受配体控制.在优化条件下,多种取代的 2,4-二氯吡啶和相关化合物发生交叉偶联形成 C4-C (Sp2)和 C4-C (Sp3)使用有机硼,-锌和-镁试剂进行键合.这种方法的合成效用在将 C4 选择性交叉偶联与随后的亲核芳族取代反应相结合的多步合成中得到了强调.本文中的大部分产品 (71%) 以前没有报道过,强调了这种方法打开未充分探索的化学空间的能力.值得注意的是,我们发现无配体的"jeffery"条件将 Suzuki 偶联的 C4 选择性提高了一个数量级 (>99:1).这些无配体条件使 2,5-二氯吡啶和
Doi:10.1021/acs.Joc.2C00665

专利信息

专利号:US-2025115551-A1
优先权日:2023-10-03
标 题:Synthesis of ras inhibitors
发明人：LI YI; MENDOZA BENJAMIN; NAGANATHAN SRIRAM; WANG ROSS; YI YI; BALLMER STEVEN G; DAVIDSON JAMES; HUANG XIAOJUN
权利人:REVOLUTION MEDICINES INC
摘要:The present invention relates to Ras inhibitors, intermediates in the synthesis thereto, and methods for preparing the Ras inhibitors and the intermediates.

专利号:US-11466046-B2
优先权日:2014-10-08
标题 :14-membered ketolides and methods of their preparation and use
发明人：MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.

专利号:US-6340751-B1
优先权日:1998-07-24
标 题 :Process for the preparation of 4-substituted azetidinone derivatives
发明人：SAITO TAKAO; MURAYAMA TOSHIYUKI; MATSUMOTO TAKAJI; MIURA TAKASHI
权利人:TAKASAGO PERFUMERY CO LTD
摘要:Disclosed is a process for the preparation of a 4-substituted azetidinone derivative, which comprises reacting an azetidinone derivative and an amide compound in the presence of a magnesium compound such as those represented by the following formulas (II): n and (IV): n represented by the following formula (III): n n n MgR 5 R 6   (III) n n n wherein R 5 represents a C 1-12 alkyl group, a C 2-5 alkenyl group, a 5- to 8-membered alicyclic group which may be substituted by a lower C 1-4 alkyl group, a phenyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom or a benzyl group which may be substituted by a lower C 1-4 alkyl group, a lower C 1-4 alkoxy group or a halogen atom, and R 6 represents a halogen atom, a methanesulfonyloxy group, a benzenesulfonyloxy group, a p-toluenesulfonyloxy group, a trifluoromethanesulfonyloxy group, an acetoxy group which may be substituted by a halogen atom or a cyano group or an OR 7 group (R 7 representing a lower C 1-4 alkyl group, a substituted or unsubstituted phenyl group or a substituted or unsubstituted benzyl group). The process provides an industrially excellent process for the preparation of a 4-substituted azetidinone derivative which permits the selective preparation of an intermediate for the synthesis of a carbapenem antibacterial agent having a desired 1-β′ configuration.

专利号:US-2007173517-A1
优先权日:2006-01-20
标 题:Synthesis of 6,7-Dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides
发明人：WIRTH THOMAS; KROEBER JUTTA; NICOLA THOMAS; RAPP ARMIN; GUTHEIL DIETER; ORLICH SIMONE A; WANG XIAO-JUN; KRISHNAMURTHY DHILEEPKUMAR
权利人:WIRTH THOMAS; KROEBER JUTTA; NICOLA THOMAS; RAPP ARMIN; GUTHEIL DIETER; ORLICH SIMONE A; WANG XIAO-JUN; KRISHNAMURTHY DHILEEPKUMAR
摘要:Disclosed is an improved multi-step process for preparing a compound of Formula I: n n nwherein R 1 to R 3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.

专利号:US-7470795-B2
优先权日:2004-07-27
标 题:Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides
发明人：WANG XIAO-JUN; WIRTH THOMAS; NICOLA THOMAS; ZHANG LI; FRUTOS ROGELIO PEREZ; XU YIBO; KRISHNAMURTHY DHILEEPKUMAR; NUMMY LAURENCE JOHN; VARSOLONA RICHARD J; SENANAYAKE CHRIS HUGH; KROEBER JUTTA; REEVES DIANA
权利人:BOEHRINGER INGELHEIM PHARMA; BOEHRINGER INGELHEIM INT
摘要:Disclosed is a multi-step process for preparing a compound of Formula I: n nwherein R 1 to R 3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.

专利号:US-8487108-B2
优先权日:2005-11-14
标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors
发明人：BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T
权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC
摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.