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1. 发明申请

US20080154063A1 Compounds and methods for amino-alkylenediol synthesis 审中-公开
标题翻译：氨基亚烷基二醇合成的化合物和方法
公开(公告)号：US20080154063A1
公开(公告)日：2008-06-26
申请号：US12004190
申请日：2007-12-20
申请人： Robert O. Cain , Hendrik Moorlag , Charles E. Tucker , Jim-Wah Wong
发明人： Robert O. Cain , Hendrik Moorlag , Charles E. Tucker , Jim-Wah Wong
IPC分类号： C07C215/10 , C07C213/00 , C07C215/20
CPC分类号： C07C213/02 , C07C215/16 , Y02P20/55 , C07C215/10
摘要： A method of making an amino-alkylenediol and intermediate compounds useful in the method is disclosed. The method includes preparing a first intermediate compound comprising an aminoalkylene diol wherein a protecting group is linked to the amino functionality, and optionally, preparing a second intermediate compound comprising a salt of the first intermediate compound.The first intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, and Z is a protecting group.The second intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, TsO− is toluene sulfonate, and Z is a protecting group.
摘要翻译：公开了制备用于该方法的氨基亚烷基二醇和中间体化合物的方法。该方法包括制备包含氨基亚烷基二醇的第一中间体化合物，其中保护基与氨基官能团连接，任选地，制备包含第一中间体化合物的盐的第二中间体化合物。第一中间体化合物具有其中R为具有2至20个碳原子的二价亚烷基，X和Y独立地为二价连接部分或单键的结构，Z为保护基。第二中间体化合物具有其中R是具有2至20个碳原子的二价亚烷基的结构，X和Y独立地是二价连接部分或单键，TsO - 是甲苯磺酸酯，和 Z是保护组。

2. 发明授权

US6103901A Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效
标题翻译：制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US6103901A
公开(公告)日：2000-08-15
申请号：US121446
申请日：1998-07-23
申请人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
发明人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
IPC分类号： C12N11/08 , C07D473/18 , C12N9/20 , C12N9/80 , C12P17/18 , C07B51/00
CPC分类号： C07D473/18 , Y02P20/55
摘要： Intermediates of Formula (III) ##STR1## wherein P.sup.1 is hydrogen or an amino-protecting group, R is lower alkyl, allyl or aralkyl, and Z is hydrogen, lower alkyl, aryl or aralkyl; and Formula (VI) ##STR2## wherein P.sup.1 is hydrogen or an amino-protecting group, P.sup.2 is an amino protecting group, and Z is hydrogen, lower alkyl, aryl or aralkyl, are useful in a novel process for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol (ganciclovir). The mono-L-valine ester of ganciclovir and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.
摘要翻译：其中P1为氢或氨基保护基的式（III）中间体，R为低级烷基，烯丙基或芳烷基，Z为氢，低级烷基，芳基或芳烷基; 和式（VI）其中P1是氢或氨基保护基，P2是氨基保护基，Z是氢，低级烷基，芳基或芳烷基，可用于制备单-L-缬氨酸酯的新方法的2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇（更昔洛韦）。更昔洛韦的单-L-缬氨酸酯及其药学上可接受的盐具有改善吸收的抗病毒剂的价值。

3. 发明授权

US5840890A Process for preparing a 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol derivative 失效
标题翻译：制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇衍生物的方法
公开(公告)号：US5840890A
公开(公告)日：1998-11-24
申请号：US775424
申请日：1997-01-09
申请人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
发明人： Humberto B. Arzeno , Eric R. Humphreys , Jim-Wah Wong , Christopher R. Roberts
IPC分类号： C12N11/08 , C07D473/18 , C12N9/20 , C12N9/80 , C12P17/18 , C07B51/00
CPC分类号： C07D473/18 , Y02P20/55
摘要： Process and novel intermediates for preparing the mono-L-valine ester of 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol ganciclovir) and its pharmaceutically acceptable salts. The present process and monoester intermediates provide for mono-esterification by an L-valine derivative, resulting in a monocarboxylate-monovalinate which is then selectively hydrolyzed under basic or enzymatic conditions to give the monovaline ester of ganciclovir in high yield and purity. These products are of value as antiviral agents with improved absorption.
摘要翻译：用于制备2-（2-氨基-1,6-二氢-6-氧代 - 嘌呤-9-基）甲氧基-1,3-丙二醇更昔洛韦的单-L-缬氨酸酯的方法和新型中间体及其药学上可接受的盐。本方法和单酯中间体通过L-缬氨酸衍生物提供单酯化，得到单羧酸酯 - 单戊酸酯，然后在碱性或酶条件下选择性水解，以高产率和纯度得到更昔洛韦的单戊酸酯。这些产品具有改善吸收的抗病毒药物的价值。

4. 发明授权

US5811556A Preparation of mibefradil via a naphthalenylacetic acid 失效
标题翻译：通过萘乙酸制备米非拉迪
公开(公告)号：US5811556A
公开(公告)日：1998-09-22
申请号：US60168
申请日：1998-04-14
申请人： Peter J. Harrington , Jim-Wah Wong
发明人： Peter J. Harrington , Jim-Wah Wong
IPC分类号： C07D235/14
CPC分类号： C07D235/14
摘要： A method of preparing 2-�2-{�3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate comprises contacting (6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid or an activated derivative of (6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)acetic acid with �3-(1H-benzimidazol-2-yl)propyl!methylamine to form N-�3-(1H-benzimidazol-2-yl) propyl!-2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3 ,4-tetrahydronaphthalen-2-yl)-N-methylacetamide, reducing this to 2-�2-{�3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1, 2,3,4-tetrahydronaphthalen-2-ol, and treating the 2-�2-{�3-(1H-benzimidazol-2-yl) propyl!-methylamino}ethyl!-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-ol with methoxyacetic acid or an activated derivative of methoxyacetic acid. The invention is particularly applicable to the preparation of mibefradil, (1S,2S)-2-�2-{�3-(1H-benzimidazol-2-yl)propyl!methylamino}-ethyl!-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate, and its dihydrochloride salt. N-�3-(1H-benzimidazol-2yl)propyl!-2-(6-fluoro-2-hydroxy-1-isopropyl-1, 2,3,4-tetrahydronaphthalen-2-yl)-N-methylacetamide is new.
摘要翻译：制备2- [2 - {[3-（1H-苯并咪唑-2-基）丙基]甲基氨基}乙基] -6-氟-1-氟-2-丙基-1,2,3,4-四氢化萘-2-酮的方法，（6-氟-2-羟基-1-异丙基-1,2,3,4-四氢萘-2-基）乙酸或活性衍生物（6-氟-2-羟基-1-异丙基 -1,2,3,4-四氢萘-2-基）乙酸与[3-（1H-苯并咪唑-2-基）丙基]甲胺反应，形成N- [3-（1H-苯并咪唑-2-基）丙基 ] -2-（6-氟-2-羟基-1-异丙基-1,2,3,4-四氢萘-2-基）-N-甲基乙酰胺，将其还原成2- [2 - {[3-（1H - 苯并咪唑-2-基）丙基]甲基氨基}乙基] -6-氟-1-氟丙基-1,2,3,4-四氢萘-2-醇，并处理2- [2 - {[3-（ 1H-苯并咪唑-2-基）丙基] - 甲基氨基}乙基] -6-氟-1-异丙基-1,2,3,4-四氢萘-2-醇与甲氧基乙酸或甲氧基乙酸的活化衍生物反应。本发明特别适用于制备三烯丙基（1S，2S）-2- [2 - {[3-（1H-苯并咪唑-2-基）丙基]甲基氨基} - 乙基] -6-氟-1- 异丙基-1,2,3,4-四氢萘-2-基甲氧基乙酸酯及其二盐酸盐。 N- [3-（1H-苯并咪唑-2-基）丙基] -2-（6-氟-2-羟基-1-异丙基-1,2,3,4-四氢化萘-2-基）-N-甲基乙酰胺是新的。

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