2-(Diethylamino)-1-((Triethylsilyl)Ethynyl)Cyclohexan-1-Ol置于氢氧化钾体系中,化学反应生成三乙基矽乙炔 参考文献:Malinovskii,M.S. Et Al.,Soviet Progress In Chemistry,1973,Vol. 39,# 12,P. 56-58 标题:Malinovskii,M.S. Et Al.,Soviet Progress In Chemistry,1973,Vol. 39,# 12,P. 56-58
专利号:US-11873305-B2 优先权日:2020-06-30 标题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds 发明人:ZHANG HAIMING; XU JIE; WUITSCHIK GEORG; ANGELAUD REMY; HEROLD SEBASTIAN; STUTZ ALFRED; BRUETSCH TOBIAS; BURKHARD JOHANNES 权利人:GENENTECH INC; HOFFMANN LA ROCHE 摘要:Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-8735589-B2 优先权日:2009-08-20 标题:Process for the synthesis of naratriptan 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; CHIKHALIKAR SANDIP VASANT; GHAGARE MARUTI 权利人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; CHIKHALIKAR SANDIP VASANT; GHAGARE MARUTI; CIPLA LTD 摘要:The present invention relates to a process for preparing naratriptan or a salt thereof, the process comprising: (a) reacting a compound of formula (3) with a compound of the formula HCCR n nwherein Z is a protecting group, Y is a leaving group and R is a trialkyl silyl group, a trialkylstannyl group or a zinc (II) halide, to obtain the compound of formula (4); (b) converting the compound of formula (4) to a compound of formula (5)n n nwherein Z′ is hydrogen or a benzyl group; (c) converting the compound of formula (5) to naratriptan; and (d) optionally converting naratriptan to a salt thereof. The present invention also provides novel compounds (3) and (4) and processes for their preparation.
专利号:US-5079349-A 优先权日:1989-02-10 标题 :Trimethylsilyl acetylene compounds, their preparation and their use in the preparation of daunomycinone derivatives 发明人:SCHEEREN JOHAN W; DE BIE JOANNES F M; DE VOS DIRK 权利人:PHARMACHEMIE BV 摘要:The invention relates to novel compounds of the formulae wherein S is H, alkyl or alkoxy and R is a good leaving group, and to the preparation of these compounds in a stereospecific manner to obtain a configuration wherein OH at C-3 and OR at C-1 are in the cis-position, which compounds can be used for the synthesis of daunomycinone and derivatives thereof. Daunomycinone can be used for the preparation of daunomycin and adriamycin.
专利号:US-2024174678-A1 优先权日:2020-06-30 标 题 :Processes for synthesis of substituted indole intermediates for the synthesis of serd compounds