CAS: 4670-10-4; 2-(3,5-Dimethoxyphenyl)Acetic Acid

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3,5-二甲氧基苯甲醛置于盐酸,硼烷四氢呋喃络合物,甲基磺酰氯,三乙胺体系中,用 四氢呋喃,N-甲基吡咯烷酮,水 作为反应溶剂,化学反应 22.0H,反应生成 (3,5-二甲氧基苯基)乙酸
参考文献:糖肽类抗生素的突变合成:万古霉素 Ab 环氨基酸 3,5-二羟基苯基甘氨酸的变异
标题:糖肽类抗生素的突变合成:万古霉素 Ab 环氨基酸 3,5-二羟基苯基甘氨酸的变异
摘要:在突变合成方法中,万古霉素型糖肽抗生素生产者 Amycolatopsis Balhimycina 的 Deltadpga 突变体在 3,5-二羟基苯基甘氨酸 (Dpg) 的合成中存在缺陷,补充了合成的 Dpg 类似物以获得相应的修饰糖肽.空间上要求更高的 3,5-二取代甲氧基衍生物以及单取代 Dpg 类似物被接受为底物.这些事实表明,空间和电子要求在几种情况下足以使 Ab 环氧化闭合,从而导致产生新的抗生素活性糖肽衍生物.结果代表了评估肽次生代谢物突变合成潜力的进一步步骤.
DOI:10.1021/ja0499389

专利信息

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-9783549-B2
优先权日:2013-11-04
标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B
发明人：FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) 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., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.

专利号:US-2024024497-A1
优先权日:2020-08-06
标 题:Methods for the synthesis of protein-drug conjugates
发明人：BORCHARDT ALLEN; HUGHES ROBERT MICHAEL
权利人:CIDARA THERAPEUTICS INC
摘要:The present invention relates to methods for the synthesis of conjugates useful for the treatment of viral infections, e.g., conjugates containing inhibitors of viral neuraminidase (e.g., zanamivir or an analog thereof) linked to an Fc domain monomer.

专利号:WO-2024137329-A1
优先权日:2022-12-20
标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof
发明人：HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR
权利人:ALEXION PHARMA INC
摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.