尿酸 反应生成 可可碱 参考文献:Bredereck Et Al.,Chemische Berichte,1950,Vol. 83,P. 201,209 标题:Bredereck Et Al.,Chemische Berichte,1950,Vol. 83,P. 201,209
专利信息
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-11639349-B2 优先权日:2020-05-28 标题:Stereoselective synthesis of intermediate for preparation of heterocyclic compound 发明人:CHEN WEN-CHANG; HSU HAN-PEI; CHOU SHAN-YEN; CHUANG SHIH-CHIEH; YEN CHI-FENG 权利人:TAI GEN BIOTECHNOLOGY CO LTD; TAIGEN BIOPHARMACEUTICALS CO BEIJING LTD; TAIGEN BIOTECHNOLOGY CO LTD 摘要:Provided is a stereoselective synthesis of an intermediate for the preparation of the heterocyclic derivative as a Cap-dependent endonuclease inhibitor. The synthesis process has the advantages of simple operation, higher yield and relatively controllable steroselectivity, such that it is suitable for large-scale production.
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-11912647-B2 优先权日:2020-05-22 标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation 发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS 权利人:UNIV GEORGIA 摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.
1: Berends LM, van der Velpen V, Cassidy A. Flavan-3-ols, theobromine, and the effects of cocoa and chocolate on cardiometabolic risk factors. Curr Opin Lipidol. 2015 Feb;26(1):10-9. doi: 10.1097/MOL.0000000000000144. Review. doi: 10.1007/978-3-642-13443-2_7. Review. Review. Review. Review. Review.
合成参考文献
参考文献:10.1007/s00216-010-3506-1 摘要:Carvalho JJ, Weller MG, Panne U, Schneider RJ. A highly sensitive caffeine immunoassay based on a monoclonal antibody. Analytical and Bioanalytical Chemistry. 2010 Feb 16;396(7):2617–28. doi: 10.1007/s00216-010-3506-1. 参考文献:10.1136/thx.2010.156695 摘要:Ibrahim B, Basanta M, Cadden P, Singh D, Douce D, Woodcock A, Fowler SJ. Non-invasive phenotyping using exhaled volatile organic compounds in asthma. Thorax. 2011 Sep;66(9):804–9. doi: 10.1136/thx.2010.156695.