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1. 发明申请

WO02085848A8 SYNTHESIS OF PANCRATISTATIN PRODRUGS 审中-公开
标题翻译：人参皂苷前体的合成
公开(公告)号：WO02085848A8
公开(公告)日：2003-05-30
申请号：PCT/US0211964
申请日：2002-04-17
申请人： UNIV ARIZONA STATE , PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
发明人： PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
IPC分类号： A61P31/14 , A61P35/00 , C07D453/04 , C07D491/04 , C07F9/6561 , C07D471/00
CPC分类号： C07F9/6561 , Y02P20/55
摘要： A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.
摘要翻译：（+） - pancratistatin磷酸酯前药2a的新的和有效的合成已经完成。（+） - pancratistatin（1a）的选择性保护（四乙酸酯4）之后，用二苄基氯亚磷酸酯（由二苄基亚磷酸酯原位制备）磷酸化（至5）。乙酸酯（含有甲醇钠）和苄基（通过氢解）保护基团的裂解随后与2当量的甲醇钠反应提供了良好收率的（+） - pancratistatin-磷酸二钠（2a）。前药（2a）的收率进一步增加是通过避免最终纯化步骤中的加热来实现的。还合成了十四个（2b-o）另外的金属和铵衍生的磷酸酯前药。

2. 发明申请

WO2003059855A1 SYNTHESIS OF COMBRETASTATIN A-2 PRODRUGS 审中-公开
标题翻译：化合物A-2 PRODRUGS的合成
公开(公告)号：WO2003059855A1
公开(公告)日：2003-07-24
申请号：PCT/US2002/040885
申请日：2002-12-20
申请人： ARIZONA BOARD OF REGENTS , PETIT, George, R. , MOSER, Bryan, R.
发明人： PETIT, George, R. , MOSER, Bryan, R.
IPC分类号： C07C41/06
CPC分类号： C07F9/65517 , C07C43/23 , C07F9/12 , Y02P20/55
摘要： The original synthesis of combretastatin A-2 (1a) was modified to provide an efficient scale-up procedure for obtaining this antineoplastic stilbene. Subsequent conversion to a useful prodrug was accomplished by phosphorylation employing in situ formation of dibenzylchlorophosphite followed 30 by cleavage of the benzyl ester protective groups with bromotrimethylsilane to afford phosphoric acid intermediate 11. The latter was immediately treated with sodium methoxide to complete a practical route to the disodium phosphate prodrug (2a). The phosphoric acid precursor (11) of phosphate 2a was employed in a parallel series of reactions to produce a selection of metal and ammonium cation prodrug candidates. Each of the phosphate salts (2a-q) was evaluated with respect to relative solubility behavior, cancer cell growth inhibition, and antimicrobial activity.
摘要翻译：改变了考布他汀A-2（1a）的原始合成，为获得这种抗肿瘤的二苯乙烯提供了有效的放大方法。随后转化为有用的前体药物是通过使用原位形成二氯苄基亚磷酸酯进行磷酸化，然后通过用溴代三甲基甲硅烷裂解苄酯保护基来提供磷酸中间体11来完成的。后者立即用甲醇钠处理以完成实际路线磷酸二钠前药（2a）。磷酸二烷基酯（11）以平行的一系列反应方式使用，以产生金属和铵阳离子前体药物候选物的选择。关于相对溶解行为，癌细胞生长抑制和抗微生物活性来评价磷酸盐（2a-q）中的每一种。

3. 发明申请

WO02085848A2 SYNTHESIS OF PANCRATISTATIN PRODRUGS 审中-公开
标题翻译： PANCRATISTATIN PRODRUGS的合成
公开(公告)号：WO02085848A2
公开(公告)日：2002-10-31
申请号：PCT/US0211964
申请日：2002-04-17
申请人： UNIV ARIZONA STATE , PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
发明人： PETIT GEORGE R , ORR BRIAN , DUCKI SYLVIE
IPC分类号： A61P31/14 , A61P35/00 , C07D453/04 , C07D491/04 , C07F9/6561 , C07D
CPC分类号： C07F9/6561 , Y02P20/55
摘要： A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.
摘要翻译：已经完成了（+） - 泛磷酸肌苷酸前药2a的新的和有效的合成。（+） - pancratistatin（1a）的选择性保护（四乙酸酯4），随后用二氯亚磷酸二苄基酯（由二亚磷酸酯原位制备）进行磷酸化（至5）。乙酸盐（用甲醇钠）和苄基（通过氢解）保护基团裂解，随后与两当量甲醇钠同时反应，得到良好的二钠（+） - 磷酸二钙（2a）的产率。通过在最终纯化步骤中避免热量来实现前药（2a）的产率的进一步提高。还合成了十四（2b-o）个额外的金属和铵衍生的磷酸酯前药。

4. 发明申请

WO2002085848A3 SYNTHESIS OF PANCRATISTATIN PRODRUGS 审中-公开
公开(公告)号：WO2002085848A3
公开(公告)日：2002-10-31
申请号：PCT/US2002/011964
申请日：2002-04-17
申请人： ARIZONA BOARD OF REGENTS, a body corporate of the State of Arizona acting for and on behalf of ARIZONA STATE UNIVERSITY , PETIT, George, R. , ORR, Brian , DUCKI, Sylvie
发明人： PETIT, George, R. , ORR, Brian , DUCKI, Sylvie
IPC分类号： C07D471/00
摘要： A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.

5. 发明申请

WO0118032A2 DOLASTATIN PEPTIDES 审中-公开
公开(公告)号：WO0118032A2
公开(公告)日：2001-03-15
申请号：PCT/US0024658
申请日：2000-09-08
申请人： BASF AG , UNIV ARIZONA , PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
发明人： PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
IPC分类号： C07K5/02 , C07K7/02 , C07K5/00
CPC分类号： C07K5/0202 , C07K5/0205 , C07K7/02
摘要： The present invention provides compounds of formula (I) where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocyclic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or -C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.
摘要翻译：本发明提供式（I）化合物，其中R 1 -R 5各自独立地为氢原子或正
或支链C 1 -C 6烷基; A是甲硫氨酰基，苯丙氨酰或苯基甘氨酰残基; n为0或1; R6是氢原子; 并且R 7是碳环基，芳基，C 1 -C 4 - 烷基，吡啶基烷基或杂环基。在另一个实施方案中，R 6为苄基或-C（O）OR 8，其中R 8为C 1 -C 6烷基，R 7为杂芳族基团，例如2-噻唑基。

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