专利号:US-8642809-B2 优先权日:2007-09-25 标 题:Methods of synthesis of certain hydroxamic acid compounds 发明人:REISCH HELGE A; LEEMING PETER; RAJE PRASAD S 权利人:REISCH HELGE A; LEEMING PETER; RAJE PRASAD S; TOPOTARGET UK LTD 摘要:The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PUR C ) optional purification; (AAA) alkenyl-acid addition, comprising: either (i): the steps of, in order: (ACAEA) alkenyl-carboxylic acid ester addition; (PUR E ) optional purification; and (CAD) carboxylic acid deprotection; or (ii): the step of: (ACAA) alkenyl-carboxylic acid addition; (PUR F ) optional purification; (HAF) hydroxamic acid formation; and (PUR G ) optional purification.
专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
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-9409945-B2 优先权日:1999-10-04 标 题 :Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery 发明人:DESLONGCHAMPS PIERRE; DORY YVES; BERTHIAUME GILLES; OUELLET LUC; LAN RUOXI 权利人:OCERA THERAPEUTICS INC 摘要:A library of macrocyclic compounds of the formula (I) n n n n n n n n n n n n where part (A) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) y — bivalent radical or a covalent bond; n where part (B) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) z — bivalent radical, or a covalent bond; n where part (C) is a n n n n n n n n n n n n n n n n  bivalent radical, a —(CH 2 ) t — bivalent radical, or a covalent bond; and n where part (T) is a —Y-L-Z— radical wherein Y is CH 2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.
专利号:US-9802953-B2 优先权日:2007-10-03 标 题 :Intermediates and methods for the synthesis of halichondrin B analogs 发明人:CHASE CHARLES E; ENDO ATSUSHI; FANG FRANCIS G; LI JING 权利人:EISAI R&D MAN CO LTD 摘要:Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
专利号:US-6723853-B2 优先权日:2001-08-27 标 题 :Intermediates and methods of preparation of intermediates in the enantiomeric synthesis of (20R)homocamptothecins and the enantiomeric synthesis of (20R)homocamptothecins 发明人:CURRAN DENNIS P; GABARDA ANA E 权利人:UNIV PITTSBURGH 摘要:A method of synthesizing a compound having the formula: n from a compound having the formula: n wherein R 1 is hydrogen, fluorine, chlorine or SiR 5 R 6 R 7 , wherein R 5 , R 6 , and R 7 are independently the same or different an alkyl group or an aryl group, R 2 is an alkyl group, R 3 is a protecting group, R 4 is an alkyl group, an allyl group, a propargyl group —CO 2 H, or a benzyl group, R 8 is —CO 2 R 10 , wherein R 10 is an alkyl group or an aryl group, X 1 is OH and X 2 is H, includes the step of exposing compound (III) to at least one of an organic acid or an inorganic acid. A compound has the general formula (III).
摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 40. 摘要:Arai, T., Science of Synthesis Knowledge Updates, (2010) 4, 231. 摘要:Christmann, M., Science of Synthesis: Asymmetric Organocatalysis, (2012) 1, 441. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).