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1.发明公开Reagents and methods for the beta-keto amide synthesis of a synthetic precursor to immunological adjuvant e6020 审中-公开试剂和方法免疫Ajduvans E6020的合成前体的β-酮酰胺合成
公开(公告)号：EP2565179A1
公开(公告)日：2013-03-06
申请号：EP12178716.2
申请日：2008-12-18
发明人： Decosta, Bruce , Fang, Francis, G. , Foy, James, E. , Hawkins, Lynn , Lemelin, Charles , Niu, Xiang , Wu, Kuo-Ming
IPC分类号： C07C235/70 , C07C231/00 , C07F9/24 , C07C235/74 , C07C235/76
CPC分类号： C07F9/091 , C07C235/74 , C07C235/76 , C07F9/2408 , Y02P20/55
摘要： This invention relates to the synthesis for a precursor of E6020, compound 26, via a β-keto amide alcohol intermediate, compound 22. The synthesis reacts compound 22 with compound 25 and the resultant intermediate is oxidized to produce compound 26, the precursor to E6020. Compounds 22 and 25, and their crystalline forms, represent separate embodiments of the invention. The invention also relates to compounds of formulas (3) and (4) and processes for their preparation. The β-keto amide alcohol intermediate compound 22 is a compound of formula (3). Compound 25 is a compound of formula (4).
摘要翻译： 本发明涉及合成对E6020，化合物26的前体，经由²α-酮酰胺醇中间体，化合物22的合成化合物发生反应22化合物25和将所得的中间被氧化以产生化合物26，前体E6020 ， 化合物22和25，及其结晶形式，代表本发明的单独的实施方案。 因此，本发明涉及式（3）和（4）和它们的制备方法的化合物。 所述²α-酮酰胺醇中间体化合物22是式（3）的化合物。 化合物25为通式（4）的化合物。
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2.发明授权Intermediates for the synthesis of halichondrin B analogs 有权Zwischenprodukte zur Synthese von Halichondrin-B-Analoga
公开(公告)号：EP2578576B1
公开(公告)日：2016-03-23
申请号：EP12191294.3
申请日：2008-10-03
发明人： Chase, Charles , Endo, Atsushi , Fang, Francis, G. , Li, Jing
IPC分类号： C07D307/28 , C07D307/33 , C07D493/08 , C07D493/18
CPC分类号： C07D493/20 , C07D307/20 , C07D307/26 , C07D307/28 , C07D307/33 , C07D309/16 , C07D405/06 , C07D405/14 , C07D493/04 , C07D493/08 , C07D493/18 , C07D493/22 , Y02P20/55
摘要： The following intermediates for the synthesis of halichondrin B analogs are described: Compound AU, Compound AR, or a composition comprising a compound having the formula:
摘要翻译： 描述了用于合成软组蛋白B类似物的以下中间体：化合物AU，化合物AR或包含具有下式的化合物的组合物：
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公开(公告)号：EP2578576A1
公开(公告)日：2013-04-10
申请号：EP12191294.3
申请日：2008-10-03
发明人： Chase, Charles , Endo, Atsushi , Fang, Francis, G. , Li, Jing
IPC分类号： C07D307/28 , C07D307/33 , C07D493/08 , C07D493/18
CPC分类号： C07D493/20 , C07D307/20 , C07D307/26 , C07D307/28 , C07D307/33 , C07D309/16 , C07D405/06 , C07D405/14 , C07D493/04 , C07D493/08 , C07D493/18 , C07D493/22 , Y02P20/55
摘要： The following intermediates for the synthesis of halichondrin B analogs are described:
Compound AU,
Compound AR,
or a composition comprising a compound having the formula:-
公开(公告)号：EP2578576B9
公开(公告)日：2016-09-14
申请号：EP12191294.3
申请日：2008-10-03
发明人： Chase, Charles , Endo, Atsushi , Fang, Francis, G. , Li, Jing
IPC分类号： C07D307/28 , C07D307/33 , C07D493/08 , C07D493/18
CPC分类号： C07D493/20 , C07D307/20 , C07D307/26 , C07D307/28 , C07D307/33 , C07D309/16 , C07D405/06 , C07D405/14 , C07D493/04 , C07D493/08 , C07D493/18 , C07D493/22 , Y02P20/55
摘要： The following intermediates for the synthesis of halichondrin B analogs are described: Compound AU, Compound AR, or a composition comprising a compound having the formula:
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