CAS: 1121-89-7; Piperidine-2,6-Dione

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哌啶酮置于二甲基二环氧乙烷体系中,用 丙酮 用作溶剂,化学反应 48.0H,以99%的收率获得戊二酰亚胺
参考文献:杂解(2 E)与均解(1 E)氧化反应性:二环氧乙烷对内酰胺的氧化中的nh与ch转换
标题:杂解(2 E)与均解(1 E)氧化反应性:二环氧乙烷对内酰胺的氧化中的nh与ch转换
摘要:二恶英是强大的氧化剂,可通过两种不同的机制起作用:1)均溶(h提取和氧回弹)和2)杂溶(亲电子氧化).迄今为止,已经报道了底物的性质决定了反应模式,而与所使用的二环氧乙烷无关.在此,我们报道了前所未有的情况,其中二环氧乙烷的性质决定了氧化化学选择性.特别是,在内酰胺从二甲基二环氧乙烷(ddo)转移到甲基(三氟甲基)二环氧乙烷(tfdo)的内酰胺氧化中观测到了从ch到nh的转换.一项物理有机化学研究,将氧化与其他两种二氧杂环戊烷甲基(氟甲基)二环氧乙烷,Mfdo和甲基(二氟甲基)二环氧乙烷相结合,通过计算研究,Dfdo指出二恶英类化合物具有稳定同源或杂合途径的多种能力.
Doi:10.1002/chem.201604507

专利信息

专利号:US-7230101-B1
优先权日:2002-08-28
标 题:Synthesis of methotrexate-containing heterodimeric molecules
发明人：MURTHI KRISHNA K; SMITH CHASE C
权利人:GPC BIOTECH INC
摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:

专利号:US-11542269-B2
优先权日:2018-01-03
标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof
发明人：CHOI HYEONG-WOOK; FANG FRANCIS G
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

专利号:US-10913749-B2
优先权日:2015-05-07
标 题 :Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides
发明人：FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Horner-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

专利号:US-11136335-B2
优先权日:2016-06-30
标题:Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof
发明人：CHASE CHARLES E; CHOI HYEONG-WOOK; ENDO ATSUSHI; FANG FRANCIS G; KIM DAE-SHIK
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.

专利号:US-2004249114-A1
优先权日:2001-02-06
标题 :Methods of synthesis of polysuccinimide or polyaspartate by end capping polymerization
发明人：SWIFT GRAHAM; REDLICH GEORGE H; WEHBY JOHN NOLAN
摘要:Disclosed are methods of synthesis of homopolymers or copolymers containing succinimide or aspartate moieties formed in the presence of an end capping initiator. Also disclosed are methods of isolating, compounding, stabilizing and processing the homopolymers and copolymers.

专利号:US-2006211843-A1
优先权日:2001-02-06
标题:Methods of synthesis of poly(succinimide-aspartate) polysuccinimide or polyaspartate by end capping polymerization
发明人：SWIFT GRAHAM; REDLICH GEORGE H
权利人:SWIFT GRAHAM; REDLICH GEORGE H
摘要:Disclosed are methods of synthesis of homopolymers or copolymers containing succinimide or aspartate moieties formed in the presence of an end capping initiator. Also disclosed are methods of isolating, compounding, stabilizing and processing the homopolymers and copolymers.