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1. 发明授权

US5247089A Method of making intermediates useful for the manufacture of camptothecin and camptothecin analogs 失效
标题翻译：制备适于制造喜树碱和喜树碱类似物的中间体的方法
公开(公告)号：US5247089A
公开(公告)日：1993-09-21
申请号：US927219
申请日：1992-08-10
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04 , C07D491/052 , C07D491/22
CPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04
摘要： Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.t may be H, loweralkyl, loweralkoxy, or halo: R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.
摘要翻译：式I的化合物按照下列方案制备：其中R可以是低级烷基; R 2可以是H，低级烷基，低级烷氧基或卤素：R 2，R 3，R 4和R 5可以各自独立地为H，氨基，羟基，低级烷基，低级烷氧基，低级烷硫基，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰胺基，肼基或通过氨基 - 氮原子与A环键合的二十个标准氨基酸中的任何一个; Y是H，W和X是卤素。还公开了用于制备上述方案的起始材料的新方法和在这些方法中使用的新型中间体。

2. 发明授权

US5191082A Camptothecin intermediate and method of making camptothecin intermediates 失效
标题翻译：喜树碱中间体和制备喜树碱中间体的方法
公开(公告)号：US5191082A
公开(公告)日：1993-03-02
申请号：US927217
申请日：1992-08-10
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04 , C07D491/052 , C07D491/22
CPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04
摘要： Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.
摘要翻译：式I的化合物按照下列方案制备：其中R可以是低级烷基; R1可以是H，低级烷基，低级烷氧基或卤素; R2，R3，R4和R5可以各自独立地为H，氨基，羟基，低级烷基，低级烷氧基，低级烷硫基，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰氨基，或通过氨基氮原子与A环键合的二十个标准氨基酸中的任何一个; Y是H，W和X是卤素。还公开了用于制备上述方案的起始材料的新方法和在这些方法中使用的新型中间体。

3. 发明授权

US5162532A Intermediates and method of making camptothecin and camptothecin analogs 失效
标题翻译：中药和制备CAMPTOTHECIN和CAMPTOTHECIN模拟物的方法
公开(公告)号：US5162532A
公开(公告)日：1992-11-10
申请号：US632970
申请日：1990-12-20
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： A61K31/4745 , A61P35/02 , C07B61/00 , C07D213/64 , C07D213/69 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D471/22 , C07D491/04 , C07D491/052 , C07D491/22 , C07D519/00
CPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04
摘要： Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.
摘要翻译：式I的化合物按照下列方案制备：其中R可以是低级烷基; R1可以是H，低级烷基，低级烷氧基或卤素; R2，R3，R4和R5可以各自独立地为H，氨基，羟基，低级烷基，低级烷氧基，低级烷硫基，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰氨基，或通过氨基氮原子与A环键合的二十个标准氨基酸中的任何一个; Y是H，W和X是卤素。还公开了用于制备上述方案的起始材料的新方法和在这些方法中使用的新型中间体。

4. 发明授权

US5243050A Alkylpyridone DE ring intermediates useful for the manufacture of camptothecin and camptothecin analogs 失效
标题翻译：用于制造喜树碱和喜树碱类似物的烷基吡啶酮DE环中间体
公开(公告)号：US5243050A
公开(公告)日：1993-09-07
申请号：US969790
申请日：1992-10-29
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04 , C07D491/052 , C07D491/22
CPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04
摘要： Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.
摘要翻译：式I的化合物按照下列方案制备：其中R可以是低级烷基; R1可以是H，低级烷基，低级烷氧基或卤素; R2，R3，R4和R5可以各自独立地为H，氨基，羟基，低级烷基，低级烷氧基，低级烷硫基，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰氨基，或通过氨基氮原子与A环键合的二十个标准氨基酸中的任何一个; Y是H，W和X是卤素。还公开了用于制备上述方案的起始材料的新方法和在这些方法中使用的新型中间体。

5. 发明授权

US5475108A Camptothecin intermediates and method of making camptothecin and comptothecin analogs 失效
标题翻译：喜树碱中间体和喜树碱和喜树碱类似物的制备方法
公开(公告)号：US5475108A
公开(公告)日：1995-12-12
申请号：US114475
申请日：1993-08-31
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D491/052 , C07D491/22
CPC分类号： C07D491/22
摘要： Disclosed are new methods of making camptothecin and camptothecin analogs defined by Formula I: ##STR1## wherein R is loweralkyl; R.sub.1 is H, loweralkyl, loweralkoxy, or halo; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthiol, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom. The methods comprise cyclizing a compound of Formula IV: ##STR2## wherein X is Br or I, and Y is H, by an Aryl-to-Aryl free radical coupling reaction to yield a compound of Formula I. Compounds of Formula IV are made by alkylating a compound of Formula III: ##STR3## wherein R is loweralkyl and Y is H with a compound of Formula II-x: ##STR4## wherein X is a Br or I and V is hydroxy, by a Mitsunobu reaction to yield the compound of Formula IV.
摘要翻译：公开了由式I定义的喜树碱和喜树碱类似物的新方法：其中R是低级烷基; R1是H，低级烷基，低级烷氧基或卤素; 羟基，低级烷基，低级烷氧基，低级烷基硫醇，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰氨基，肼基或通过氨基 - 氮原子与A环结合的任何二十个标准氨基酸。所述方法包括使式IV化合物：其中X是Br或I，Y是H，通过芳基 - 芳基自由基偶合反应来环化式IV化合物，得到式I化合物。式IV化合物是通过将式III化合物：其中R是低级烷基并且Y是H，与式II-x的化合物：其中X是Br或I，V是羟基，通过 Mitsunobu反应得到式IV化合物。

6. 发明授权

US5264579A D ring intermediates for the synthesis of camptothecin and camptothecin analogs 失效
标题翻译： D环中间体用于合成喜树碱和喜树碱类似物
公开(公告)号：US5264579A
公开(公告)日：1993-11-23
申请号：US36053
申请日：1993-03-23
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04 , C07D491/052 , C07D491/22
CPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04
摘要： Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R.sub.6 is lower alkyl, R.sub.7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R.sub.8 is a compound of Formula ##STR2## wherein n is 1, 2, or 3, R.sub.11 is C.sub.1 -C.sub.4 alkyl and R.sub.12 is the same as R.sub.11, or R.sub.11 and R.sub.12 together form cyclopentane or cyclohexane, and R.sub.13 is:(a) phenyl substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl, or(b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl groups,R.sub.10 is C.sub.6 -C.sub.10 alkyl, aryl or alkyl aryl, and Y is H, F or Cl, are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.
摘要翻译：制备式XIV，XV和XVII的化合物的方法其中R6是低级烷基，R7是低级烷基，R是低级烷基，Y是H，F或Cl，R8是其中n为1,2或3的式（XVIII）化合物，R 11为C 1 -C 4烷基，R 12为R 11，R 11和R 12一起形成环戊烷或环己烷，R 13为：（a ）苯基与C 3 -C 7仲烷基或C 4 -C 7叔烷基取代1至5次，或（b）选自萘基，蒽基和菲基，任选被C 3 -C 7仲烷基或C 4 -C 12取代1至5次 -C 7叔烷基，R 10为C 6 -C 10烷基，芳基或烷基芳基，Y为H，F或Cl。这些方法可用于制备光学增强的和光学纯的形式的化合物，其可用于制备喜树碱及其类似物。

7. 发明授权

US5212317A Methods and intermediates for the assymmetric synthesis of camptothecin and camptothecin analogs 失效
标题翻译：喜树碱和喜树碱类似物的不对称合成方法和中间体
公开(公告)号：US5212317A
公开(公告)日：1993-05-18
申请号：US900650
申请日：1992-06-18
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04 , C07D491/052 , C07D491/22
CPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04
摘要： Processes for making compounds of Formulae XIV, XV, and XVII ##STR1## wherein R.sub.6 is lower alkyl, R.sub.7 is lower alkyl, R is lower alkyl, Y is H, F or Cl, R.sub.8 is a moiety of Formula XVIII ##STR2## wherein n is 1, 2, or 3, R.sub.11 is C.sub.1 -C.sub.4 alkyl and R.sub.12 is the same as R.sub.11, or R.sub.11 and R.sub.12 together form cyclopentane or cyclohexane, and R.sub.13 is:(a) phenyl substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl, or(b) selected from the group consisting of naphthyl, anthryl, and phenanthryl optionally substituted 1 to 5 times with C.sub.3 -C.sub.7 secondary alkyl or C.sub.4 -C.sub.7 tertiary alkyl groups,R.sub.10 is C.sub.6 -C.sub.10 alkyl, aryl or alkyl aryl,and Y is H, F or Cl,are disclosed. These processes can be used to make optically enhanced and optically pure forms of the compounds, which are useful in the making of camptothecin and analogs thereof.
摘要翻译：制备式XIV，XV和XVII的化合物的方法其中R6是低级烷基，R7是低级烷基，R是低级烷基，Y是H，F或Cl，R8是式XVIII的部分（XVIII）其中n为1,2或3，R11为C1-C4烷基，R12为R11，R11和R12一起形成环戊烷或环己烷，R 13为：（ a）用C 3 -C 7仲烷基或C 4 -C 7叔烷基取代1至5次的苯基，或（b）选自萘基，蒽基和菲基，任选被C 3 -C 7仲烷基取代1至5次或 C4-C7叔烷基，R10为C6-C10烷基，芳基或烷基芳基，Y为H，F或Cl。这些方法可用于制备光学增强的和光学纯的形式的化合物，其可用于制备喜树碱及其类似物。

8. 发明授权

US5200524A Camptothecin intermediates and method of making same 失效
标题翻译：喜树碱中间体及其制备方法
公开(公告)号：US5200524A
公开(公告)日：1993-04-06
申请号：US927220
申请日：1992-08-10
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/22 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04 , C07D491/052 , C07D491/22
CPC分类号： C07D213/64 , C07D215/18 , C07D215/20 , C07D215/233 , C07D215/26 , C07D215/36 , C07D215/38 , C07D215/40 , C07D215/48 , C07D491/04
摘要： Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluormethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediate employed in these processes.
摘要翻译：式I的化合物按照下列方案制备：其中R可以是低级烷基; R1可以是H，低级烷基，低级烷氧基或卤素; R2，R3，R4和R5可各自独立地为H，氨基，羟基，低级烷基，低级烷氧基，低级烷硫基，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰氨基，肼基，或通过氨基氮原子与A环键合的二十个标准氨基酸中的任何一个; Y是H，W和X是卤素。还公开了用于制备上述方案的起始材料的新方法和在这些方法中使用的新型中间体。

9. 发明授权

US5478943A Method of making intermediates for camptothecin and its analogs 失效
标题翻译：制备喜树碱及其类似物的中间体的方法
公开(公告)号：US5478943A
公开(公告)日：1995-12-26
申请号：US410729
申请日：1995-03-27
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： C07D491/052 , C07D491/22
CPC分类号： C07D491/22
摘要： Disclosed are new methods of making camptothecin and camptothecin analogs defined by Formula I: ##STR1## wherein R is loweralkyl; R.sub.1 is H, loweralkyl, loweralkoxy, or halo; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthiol, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom. The methods comprise cyclizing a compound of Formula IV: ##STR2## wherein X is Br or I, and Y is H, by an Aryl-to-Aryl free radical coupling reaction to yield a compound of Formula I. Compounds of Formula IV are made by alkylating a compound of Formula III: ##STR3## wherein R is loweralkyl and Y is H with a compound of Formula II-x: ##STR4## wherein X is a Br or I and V is hydroxy, by a Mitsunobu reaction to yield the compound of Formula IV.
摘要翻译：公开了由式I定义的喜树碱和喜树碱类似物的新方法：其中R是低级烷基; R1是H，低级烷基，低级烷氧基或卤素; 羟基，低级烷基，低级烷氧基，低级烷基硫醇，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰胺基，肼基或通过氨基氮原子与A环结合的二十个标准氨基酸中的任一个。所述方法包括使式IV化合物：其中X是Br或I，Y是H，通过芳基 - 芳基自由基偶合反应来环化式IV化合物，得到式I化合物。式IV化合物是通过将式III化合物：其中R是低级烷基并且Y是H，与式II-x的化合物：其中X是Br或I，V是羟基，通过 Mitsunobu反应得到式IV化合物。

10. 发明授权

US5254690A Alkoxymethylpyridine d-ring intermediates useful for the synthesis of camptpthecin and camptothecin analogs 失效
标题翻译：用于合成喜树碱和喜树碱类似物的烷氧基甲基吡啶d环中间体
公开(公告)号：US5254690A
公开(公告)日：1993-10-19
申请号：US17026
申请日：1993-02-12
申请人： Daniel L. Comins , Matthew F. Baevsky
发明人： Daniel L. Comins , Matthew F. Baevsky
IPC分类号： B23K10/00 , C07D491/052 , H05H1/34 , C07D213/64
CPC分类号： H05H1/34 , B23K10/00 , H05H2001/3457
摘要： Compounds of Formula I ##STR1## are made in accordance with the following scheme: ##STR2## wherein R may be loweralkyl; R.sub.1 may be H, loweralkyl, loweralkoxy, or halo; R.sub.2, R.sub.3, R.sub.4, and R.sub.5 may each independently be H, amino, hydroxy, loweralkyl, loweralkoxy, loweralkylthio, di(loweralkyl)amino, cyano, methylenedioxy, formyl, nitro, halo, trifluoromethyl, aminomethyl, azido, amido, hydrazino, or any of the twenty standard amino acids bonded to the A ring via the amino-nitrogen atom; Y is H and W and X are halogen. Also disclosed are novel processes for making starting materials for the scheme given above, and novel intermediates employed in these processes.
摘要翻译：式I的化合物按照下列方案制备：其中R可以是低级烷基; R1可以是H，低级烷基，低级烷氧基或卤素; R2，R3，R4和R5可以各自独立地为H，氨基，羟基，低级烷基，低级烷氧基，低级烷硫基，二（低级烷基）氨基，氰基，亚甲二氧基，甲酰基，硝基，卤素，三氟甲基，氨基甲基，叠氮基，酰胺基，或通过氨基氮原子与A环键合的二十个标准氨基酸中的任何一个; Y是H，W和X是卤素。还公开了用于制备上述方案的起始材料的新方法和在这些方法中使用的新型中间体。

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