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21. 发明授权

US5688977A Method for docetaxel synthesis 失效
标题翻译：多西紫杉醇合成方法
公开(公告)号：US5688977A
公开(公告)日：1997-11-18
申请号：US616467
申请日：1996-03-19
申请人： Nicholas J. Sisti , Charles S. Swindell
发明人： Nicholas J. Sisti , Charles S. Swindell
IPC分类号： C07D305/14
CPC分类号： C07D305/14 , Y02P20/55
摘要： A method of producing docetaxel comprises the esterification of C7, C10 di-CBZ 10-deacetyl baccatin III and an N-CBZ C2'-protected 3-phenyl isoserine side chain wherein C2' is protected by a hydrogenatable benyl-type protecting group. The C7, C10 carbobenzyloxy groups are then replaced with hydrogen and the carbobenzyloxy group at the C3' nitrogen site is replaced with t-butoxycarbonyl. Finally, the resulting compound is deprotected at C2' by replacing the benzyl-type protecting group with hydrogen to produce docetaxel. The esterification preferably employs an excess, such as six equivalents, of the side chain for each equivalent of the C7, C10 di-CBZ 10-deacetyl baccatin III. Benzyloxymethyl is the preferred protecting group at C2'.
摘要翻译：制备多西紫杉醇的方法包括C7，C10二-CZZ10-脱乙酰浆果赤霉素III和N-CBZ C2'保护的3-苯基异丝氨酸侧链的酯化，其中C2'被可氢化的烯基型保护基保护。然后用氢代替C7，C10碳代苄氧基，在C3'氮位置上的苄氧羰基被叔丁氧羰基代替。最后，通过用氢代替苄基型保护基，得到的化合物在C2'脱保护，得到多西紫杉醇。对于每当量的C 7，C 10二-CZZ 10-脱乙酰浆果赤霉素III，酯化优选使用过量的，例如6当量的侧链。苄氧基甲基是C2'的优选保护基。

22. 发明授权

US5675025A Paclitaxel synthesis from precursor compounds and methods of producing the same 失效
标题翻译：紫杉醇从前体化合物的合成及其制备方法
公开(公告)号：US5675025A
公开(公告)日：1997-10-07
申请号：US483084
申请日：1995-06-07
申请人： Nicholas J. Sisti , Charles S. Swindell , Madhavi C. Chander
发明人： Nicholas J. Sisti , Charles S. Swindell , Madhavi C. Chander
IPC分类号： C07D305/14
CPC分类号： C07D305/14 , Y02P20/55
摘要： An efficient protocol for the synthesis of taxol, taxol analogs and their intermediates is described. The process includes the attachment of the taxol A-ring side chain to baccatin III and for the synthesis of taxol and taxol analogs with variable A-ring side chain structures. A rapid and highly efficient esterification of O-protected isoserine and 3-phenylisoserine acids having N-benzyoloxycarbonyl groups to the C-13 hydroxyl of 7-O-protected baccatin III is followed by a deprotection-acylation sequence to make taxol, celphalomanninne and various analogs, including photoaffinity labeling candidates.
摘要翻译：描述了用于合成紫杉醇，紫杉醇类似物及其中间体的有效方案。该过程包括紫杉醇A环侧链与浆果赤霉素III的连接以及用可变A环侧链结构合成紫杉醇和紫杉醇类似物。具有N-苯氧基羰基的O-保护的异丝氨酸和3-苯基异丝氨酸与7-O-保护的浆果赤霉素III的C-13羟基的快速和高效的酯化反应之后是脱保护酰化顺序，以制备紫杉醇，咔唑单宁和各种类似物，包括光亲和标记候选物。

23. 发明授权

US5281727A Method of using ion exchange media to increase taxane yields 失效
标题翻译：使用离子交换介质增加紫杉烷产率的方法
公开(公告)号：US5281727A
公开(公告)日：1994-01-25
申请号：US982391
申请日：1992-11-27
申请人： David R. Carver , Timothy R. Prout , Christopher T. Workman , Donia L. Henderson , Charles L. Hughes
发明人： David R. Carver , Timothy R. Prout , Christopher T. Workman , Donia L. Henderson , Charles L. Hughes
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： The present invention is a method that uses an absorption column for the cleavage and recovery of taxanes, which are not normally detected as free taxanes. The method processes a first solution that contains standard detectable taxanes and other undetectable taxane compounds to generate a second solution that contains a higher percentage of detectable standard taxane then the first solution. The first step of this method is loading a column having a first opening and a second opening with an ion exchange media. The next step is placing the first solution in the first opening of the column so that the first solution passes through the ion exchange media in the column and flows to the second opening. Thus, the taxane compounds are converted to standard taxanes by an ion exchange reaction and the second solution is formed. Then the next step is collecting, from the second opening of the column, the second solution and recovering from the second solution a larger percentage of standard taxanes then was detectable in the first solution. The ion exchange media of the present solution is an ion exchange resin. The ion exchange resin can be a mixture of an anion exchange resin and a cation exchange resin. The anion exchange resin is in the OH-form. The cation exchange resin is in the H.sup.+ form. Preferably, the ion exchange resin is alumina.
摘要翻译：本发明是使用吸收塔来分离和回收紫杉烷的方法，其通常不被视为游离紫杉烷。该方法处理含有标准可检测的紫杉烷和其他不可检测的紫杉烷化合物的第一溶液以产生含有较高百分比的可检测标准紫杉烷的第二溶液，然后是第一溶液。该方法的第一步是用离子交换介质装载具有第一开口和第二开口的柱。下一步是将第一溶液置于塔的第一开口中，使得第一溶液通过塔中的离子交换介质并流到第二开口。因此，紫杉烷化合物通过离子交换反应转化成标准紫杉烷并形成第二溶液。然后，下一步是从第二个开口开始收集第二个溶液，然后从第二个溶液中回收，然后在第一个溶液中检测到较大百分比的标准紫杉烷。本溶液的离子交换介质是离子交换树脂。离子交换树脂可以是阴离子交换树脂和阳离子交换树脂的混合物。阴离子交换树脂为OH型。阳离子交换树脂为H +形式。优选地，离子交换树脂是氧化铝。

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