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2. 发明授权

US5227479A Process for the preparation of nojirimycin and related compounds 失效
标题翻译：制备诺瑞霉素及相关化合物的方法
公开(公告)号：US5227479A
公开(公告)日：1993-07-13
申请号：US610690
申请日：1990-11-14
申请人： Peter B. Anzeveno , Laura J. Creemer
发明人： Peter B. Anzeveno , Laura J. Creemer
IPC分类号： C07D211/44 , A61K31/445 , A61P3/08 , C07H5/04 , C07H9/04 , C07H11/00 , C07H13/12
CPC分类号： C07H9/04 , C07H13/12
摘要： The present invention relates to an efficient new route for the preparation of (+)-nojirimycin and (+)-1-deoxynojirimycin which involves the stereoselective reductive amination of 1,2-O-isopropylidene-5-oxo-.alpha.-D-glucuronolactone. The reductive amination uses particular oximes of the 5-oxo compound.

3. 发明授权

US5066807A Process for the preparation of castanospermine 失效
标题翻译：制备CASTANOSPERMINE的方法
公开(公告)号：US5066807A
公开(公告)日：1991-11-19
申请号：US492507
申请日：1990-03-12
申请人： Peter B. Anzeveno , Paul T. Angell , Laura J. Creemer
发明人： Peter B. Anzeveno , Paul T. Angell , Laura J. Creemer
IPC分类号： C07D471/04 , C07D493/04 , C07D493/14
CPC分类号： C07D471/04 , C07D493/04 , C07D493/14 , Y02P20/55
摘要： Castanospermine is prepared by starting from 5-(t-BOC)amino-5-deoxy-1,2-O-isopropylidene-.alpha.-D-glucuronolactone. Two additional carbons are added to the starting material using ethyl acetate and a strong base and the resulting cyclic hemiketal is subjected to a series of reductions, with intervening removal of protecting groups, to give the castanospermine. A substituted hydroxypyrrolidinone and a substituted hydroxypyrrolidine serve as intermediates in the process.

4. 发明授权

US4532081A Synthesis of 11-deoxyprostaglandins 失效
标题翻译： 11-脱氧前列腺素的合成
公开(公告)号：US4532081A
公开(公告)日：1985-07-30
申请号：US548130
申请日：1983-11-02
申请人： William L. White , Peter B. Anzeveno
发明人： William L. White , Peter B. Anzeveno
IPC分类号： C07C255/45 , C07C121/48
CPC分类号： C07C255/45
摘要： Improved procedures and intermediates for synthesizing 11-deoxyprostaglandins wherein trans-2,3-dicarbomethoxycyclopentanone is subjected to a novel alcoholysis with .beta.,.beta.,.beta.-trichloroethanol to substitute a .beta.,.beta.,62 -trichlorocarboethoxy group at the 2-position followed by alkylation to allow for a wide range of upper side chains to be introduced at the 2-position of the cyclopentanone ring. The unwanted .beta.,.beta.,.beta.-trichlorocarboethoxy group at the 2-position can then be removed easily by a zinc induced elimination-decarboxylation sequence. Base catalyzed epimerization of the 2-position side chain to the desired trans-configuration, relative to the carbomethoxy group in the 3-position, is followed by partial reduction of the 2-hexynyl moiety of the side chain to the desired cis-olefinic group of the E.sub.2 -type 11-dioxyprostaglandins, or through total reduction to the alkane upper side chain of E.sub.1 -type-prostaglandin analogs. Modification thereafter of the carbonyl group at the 3-position of the cyclopentanone ring by a variety of reagents allows introduction of the lower side chain present in the prostaglandins themselves or a variety of other side chains derived from the 3-carboxy-, 3-hydroxymethyl- or 3-aldehyde-substituted cyclopentanone ring. From the latter, 11-deoxyprostaglandins can be prepared by known procedures.
摘要翻译：用于合成11-脱氧前列腺素的改进方法和中间体，其中反式-2,3-二甲氧基环戊酮用β，β，β-三氯乙醇进行新的醇解，以取代2位的β，β，62-三氯甲氧基，接着进行烷基化以允许在环戊酮环的2位引入宽范围的上侧链。然后可以通过锌诱导的消除 - 脱羧化顺序容易地除去2-位上不需要的β，β，β-三氯甲氧基。相对于3-位中的甲酯基，2-位侧链的碱催化差向异构化到所需的反式构型之后，将侧链的2-己炔基部分部分还原成所需的顺式 - 烯烃基团的E2型11-二氧基前列腺素，或通过总体还原为E1型前列腺素类似物的烷烃上侧链。此后，通过多种试剂在环戊酮环的3-位上的羰基进行改性，可以引入存在于前列腺素本身中的下侧链或衍生自3-羧基，3-羟甲基的各种其它侧链 - 或3-醛取代的环戊酮环。从后者可以通过已知的方法制备11-脱氧前列腺素。

5. 发明授权

US5874627A Process for preparing polyamine derivatives and intermediates thereof 失效
标题翻译：制备多胺衍生物的方法及其中间体
公开(公告)号：US5874627A
公开(公告)日：1999-02-23
申请号：US927591
申请日：1997-09-11
申请人： Paul T. Angell , John Martin , Peter B. Anzeveno
发明人： Paul T. Angell , John Martin , Peter B. Anzeveno
IPC分类号： C07C209/62 , C07C211/14 , C07D239/04 , C07C211/09
CPC分类号： C07C209/62 , C07C211/14 , C07D239/04
摘要： A process for preparing polyamines of the formula ##STR1## by selective introduction of the groups Z--CH.sub.2 -- at the terminal nitrogens from a polyamine having no nitrogen substituents by formation of bis-hexahydropyrimidine derivative, acylation, reduction of acyl group to give Z--CH.sub.2 --, and solvolysis.
摘要翻译：通过选择性地通过形成双六氢嘧啶衍生物，通过酰基取代酰基，还原酰基，在末端氮上从不具有氮取代基的多胺选择性引入基团Z-CH2-，制备式“ CH2-和溶剂解。

6. 发明授权

US4880917A Process for hydrolyzing 2,6-dideoxy-2,6-iminoheptononitrile derivatives using trifluoroacetic acid and dinitrogen tetroxide 失效
标题翻译：使用三氟乙酸和四氧化二氮水解2,6-二脱氧-2,6-亚氨基苯腈衍生物的方法
公开(公告)号：US4880917A
公开(公告)日：1989-11-14
申请号：US214229
申请日：1988-07-01
申请人： Peter B. Anzeveno , John K. Daniel , Laura J. Creemer , Paul S. Liu
发明人： Peter B. Anzeveno , John K. Daniel , Laura J. Creemer , Paul S. Liu
IPC分类号： C07H5/04 , C07D211/46 , C07D211/60 , C07H13/06 , C07H13/08 , C07H15/26
CPC分类号： C07D211/60 , C07D211/46 , C07H15/26
摘要： A procedure for the mild conversion of a carbonitrile to the corresponding carboxylic acid by first using trifluoroacetic acid in the presence of a catalytic amount of mercuric ion followed by oxidative hydrolysis with dinitrogen tetroxide is described herein. The use of this procedure in the preparation of 1,3,4,5-tetra-O-benzoyl-2,6-dideoxy-2,6-imino-D-glycero-L-gulo-heptitol hydrochloride is also described here.

7. 发明授权

US5756739A Process for preparing polyamine derivative and intermediates thereof 失效
标题翻译：制备多胺衍生物的方法及其中间体
公开(公告)号：US5756739A
公开(公告)日：1998-05-26
申请号：US818059
申请日：1997-03-14
申请人： Paul T. Angell , John Martin , Peter B. Anzeveno
发明人： Paul T. Angell , John Martin , Peter B. Anzeveno
IPC分类号： C07C209/62 , C07C211/14 , C07D239/04 , C07D403/02
CPC分类号： C07C209/62 , C07C211/14 , C07D239/04
摘要： The present invention provides a novel process for preparing polyamine derivatives and pharmaceutically acceptable salts thereof, which are useful as antineoplastic agents and to novel intermediates thereof.
摘要翻译：本发明提供一种制备多胺衍生物及其药学上可接受的盐的新方法，其可用作抗肿瘤剂及其新型中间体。

8. 发明授权

US5093501A Intermediates in a process for the preparation of castanospermine 失效
标题翻译：中间体在制备蓖麻精的过程中
公开(公告)号：US5093501A
公开(公告)日：1992-03-03
申请号：US712780
申请日：1991-06-10
申请人： Peter B. Anzeveno , Paul T. Angell , Laura J. Creemer
发明人： Peter B. Anzeveno , Paul T. Angell , Laura J. Creemer
IPC分类号： C07D471/04 , C07D493/04 , C07D493/14
CPC分类号： C07D471/04 , C07D493/04 , C07D493/14 , Y02P20/55
摘要： Castanospermine is prepared by starting from 5-(t-BOC)amino-5-deoxy-1,2-O-isopropylidene-.alpha.-D-glucuronolactone. Two additional carbons are added to the starting material using ethyl acetate and a strong base and the resulting cyclic hemiketal is subjected to a series of reductions, with intervening removal of protecting groups, to give the castanospermine. A substituted hydroxypyrrolidinone and a substituted hydroxypyrrolidine serve as intermediates in the process.
摘要翻译：通过从5-（t-BOC）氨基-5-脱氧-1,2-O-异亚丙基-α-D-葡糖醛酸内酯开始制备睾丸精。使用乙酸乙酯和强碱将两个另外的碳加入原料中，并将所得的环状半缩醛进行一系列还原，间隔地除去保护基，得到蓖麻油精。取代的羟基吡咯烷酮和取代的羟基吡咯烷在该方法中用作中间体。

9. 发明授权

US4447636A Synthesis of 11-deoxyprostaglandins 失效
标题翻译： 11-脱氧前列腺素的合成
公开(公告)号：US4447636A
公开(公告)日：1984-05-08
申请号：US376984
申请日：1982-05-10
申请人： William L. White , Peter B. Anzeveno
发明人： William L. White , Peter B. Anzeveno
IPC分类号： C07C255/45 , C07C69/74 , C07C121/48
CPC分类号： C07C255/45
摘要： Improved procedures and intermediates for synthesizing 11-deoxyprostaglandins wherein trans-2,3-dicarbomethoxycyclopentanone is subjected to a novel alcoholysis with .beta.,.beta.,.beta.-trichloroethanol to substitute a .beta.,.beta.,.beta.-trichlorocarboethoxy group at the 2-position followed by alkylation to allow for a wide range of upper side chains to be introduced at the 2-position of the cyclopentanone ring. The unwanted .beta.,.beta.,.beta.-trichlorocarboethoxy group at the 2-position can then be removed easily by a zinc induced elimination-decarboxylation sequence. Base catalyzed epimerization of the 2-position side chain to the desired trans-configuration, relative to the carbomethoxy group in the 3-position, is followed by partial reduction of the 2-hexynyl moiety of the side chain to the desired cis-olefinic group of the E.sub.2 -type 11-deoxyprostaglandins, or through total reduction to the alkane upper side chain of E.sub.1 -type prostaglandin analogs. Modification thereafter of the carbonyl group at the 3-position of the cyclopentanone ring by a variety of reagents allows introduction of the lower side chain present in the prostaglandins themselves or a variety of other side chains derived from the 3-carboxy-, 3-hydroxymethyl- or 3-aldehyde-substituted cyclopentanone ring. From the latter, 11-deoxyprostaglandins can be prepared by known procedures.
摘要翻译：用于合成11-脱氧前列腺素的改进方法和中间体，其中反式-2,3-二甲氧基环戊酮用β，β，β-三氯乙醇进行新的醇解，以在2位置替代β，β，β-三氯甲氧基，接着进行烷基化以允许在环戊酮环的2位引入宽范围的上侧链。然后可以通过锌诱导的消除 - 脱羧化顺序容易地除去2-位上不需要的β，β，β-三氯甲氧基。相对于3-位中的甲酯基，2-位侧链的碱催化差向异构化到所需的反式构型之后，将侧链的2-己炔基部分部分还原成所需的顺式 - 烯烃基团的E2型11-脱氧前列腺素，或通过总体还原为E1型前列腺素类似物的烷烃上侧链。此后，通过多种试剂在环戊酮环的3-位上的羰基进行改性，可以引入存在于前列腺素本身中的下侧链或衍生自3-羧基，3-羟甲基的各种其它侧链 - 或3-醛取代的环戊酮环。从后者可以通过已知的方法制备11-脱氧前列腺素。

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