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1,5-diisopropylcyclohexa-1,4-diene 📜1,5-Diisopropylcyclohexa-1,4-Diene 在 C36H41Irn2P(1+)*c32H12Bf24(1-),氢气体系中,用 二氯甲烷作为反应溶剂,20.0 °C,5.0 Mpa 条件下,反应 17.0H,以99%的收率获得
参考文献:二取代和三取代环烯烃的对映选择性和区域选择性 Ir 催化氢化
标题:二取代和三取代环烯烃的对映选择性和区域选择性 Ir 催化氢化
摘要:使用新型 N,P-连接的铱咪唑基催化剂(Crabtree 型)制备并评估了许多环烯烃的不对称加氢反应.这些环烯烃的多样性跨越了那些具有很少功能的环烯烃到带有强配位取代基和杂环的环烯烃.对于几乎没有官能度(高达 > 99% Ee)的底物和具有远离烯烃几个碳的官能团的底物,均观察到了优异的对映选择性.在 C=c 键附近具有羧基,醇或杂环等官能团的底物以高对映体过量(高达 > 99% Ee)氢化.还发现氢化具有区域选择性,并且通过控制反应条件,可以实现两种三取代烯烃之一的选择性加氢.此外,三取代的烯烃可以在四取代的烯烃存在下选择性氢化.
Doi:10.1021/Jacs.6B07291
专利信息
专利号:US-11220513-B2
优先权日:2015-04-30
标题:Chromium-mediated coupling and application to the synthesis of halichondrins
发明人:KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO
权利人:HARVARD COLLEGE
摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
专利号:US-11155562-B2
优先权日:2014-06-30
标 题 :Synthesis of halichondrin analogs and uses thereof
发明人:KISHI YOSHITO; UEDA ATSUSHI; YAMAMOTO AKIHIKO; KATO DAISUKE
权利人:HARVARD COLLEGE
摘要:The present invention provides halichondrin analogs, such as compounds of Formula (I). The compounds may bind to microtubule sites, thereby inhibiting microtubule dynamics. Also provided are methods of synthesis, pharmaceutical compositions, kits, methods of treatment, and uses that involve the compounds for treatment of a proliferative disease (e.g., cancer). Compounds of the present invention are particularly useful for the treatment of metastatic breast cancer, non-small cell lung cancer, prostate cancer, and sarcoma. The included methods of synthesis are useful for the preparation of compounds of Formula (I)-(III) along with naturally occurring halicondrins (e.g., halichondrin B & C, norhalichondrin A, B, & C, and homohalichondrin A, B, & C). Also included are methods for interconverting between the halichondrins, norhalichondrins, and homohalichondrins and their unnatural epimers at the C38 ketal stereocenter through the use of an acid-mediated equilibration.
专利号:US-11130764-B2
优先权日:2017-02-17
标题 :Analogs of vincamine and uses thereof
发明人:HUIGENS III ROBERT WILLIAM; NORWOOD IV VERRILL M; LUESCH HENDRIK
权利人:UNIV FLORIDA
摘要:The present disclosure provides compounds of any one of Formulae (I′), (I), (IA), (II′), (II), (IIA), (IIIA), (III″), (III′), (III), (IIIA), (IV), (V′), (V), (VI), (VII), (VIII′), (VIII), (IX′), (IX), and (X). The compounds described herein may be useful in treating and/or preventing a broad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein.
专利号:US-11498892-B2
优先权日:2017-07-06
标 题:Fe/Cu-mediated ketone synthesis
发明人:KISHI YOSHITO; YAHATA KENZO; KUMAR VEMULA PRAVEEN; VADDELA SUDHEER BABU
权利人:HARVARD COLLEGE
摘要:Provided herein are methods for preparing ketone-containing organic molecules. The methods are based on novel iron/copper-mediated (“Fe/Cu-mediatedâ€?) coupling reactions. The Fe/Cu-mediated coupling reaction can be used in the preparation of complex molecules, such as halichondrins and analogs thereof. In particular, the Fe/Cu-mediated ketolization reactions described herein are useful in the preparation of intermediates en route to halichondrins.
专利号:US-2020223863-A1
优先权日:2014-06-30
标题 :Synthesis of halichondrin analogs and uses thereof
专利号:US-2022298109-A1
优先权日:2021-03-16
标 题:Two-step synthesis of pyrrole compounds from furan compounds