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1. 发明申请

US20090203901A1 Process for preparing pyrazole functionalized benzodiazepinones 审中-公开
标题翻译：制备吡唑官能化苯并二氮杂酮的方法
公开(公告)号：US20090203901A1
公开(公告)日：2009-08-13
申请号：US12378363
申请日：2009-02-12
申请人： Peter J. Harrington , Valerie Grace Paulsen , Charles E. Tucker
发明人： Peter J. Harrington , Valerie Grace Paulsen , Charles E. Tucker
IPC分类号： C07D487/04 , C07C211/45 , C07C233/33 , C07D243/24
CPC分类号： C07D243/24 , C07C221/00 , C07C237/04 , C07D243/28 , C07D487/04 , C07C225/22
摘要： The present invention provides innovative strategies for synthesizing pyrazole ring-functionalized benzodiazepinones. Alternative intermediates and high conversion strategies for forming alpha-aminobenzophenone intermediates involve a combination of aromatic acylation, displacement of electronegative leaving groups with amine, and then N-displacement strategies to produce the desired alpha-aminobenzophenone with primary amine functionality. Reaction strategies are then provided for converting alpha-aminobenzophenones to alpha-aminoamidobenzophenone intermediates with high yield and convenient reaction strategies. These alpha-aminoamidobenzophenone intermediates are then converted into benzodiazepinones. These benzodiazepinones are then converted to pyrazole ring functionalized benzodiazepinones through a series of innovative intermediates and/or reaction strategies.
摘要翻译：本发明提供用于合成吡唑环官能化苯并二氮杂酮的创新策略。用于形成α-氨基二苯甲酮中间体的替代中间体和高转化策略涉及芳族酰化，负电离离子基团与胺的置换，然后是N-位移策略以产生具有伯胺官能团的所需α-氨基二苯甲酮的组合。然后提供反应策略，以高产率和方便的反应策略将α-氨基二苯甲酮转化为α-氨基氨基二苯甲酮中间体。然后将这些α-氨基氨基二苯甲酮中间体转化为苯并二氮杂酮。然后通过一系列创新的中间体和/或反应策略将这些苯并二氮杂酮转化成吡唑环官能化的苯并二氮杂酮。

2. 发明授权

US06552204B1 Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one 有权
标题翻译： 3,6-二烷基-5,6-二氢-4-羟基 - 吡喃-2-酮的合成
公开(公告)号：US06552204B1
公开(公告)日：2003-04-22
申请号：US09668799
申请日：2000-09-22
申请人： Peter J. Harrington , Lewis M. Hodges , Kurt Puentener , Michelangelo Scalone
发明人： Peter J. Harrington , Lewis M. Hodges , Kurt Puentener , Michelangelo Scalone
IPC分类号： C07F704
CPC分类号： C07D309/32 , C07F7/1804 , Y02P20/55
摘要： The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein. In particular, the present invention relates to a process for enantioselectively producing the &dgr;-lactone and novel intermediates disclosed herein.
摘要翻译：本发明涉及用于制备下式的δ-内酯的新方法：使用下式的酰卤：其中R1，R2 R3和X如本文所述。特别地，本发明涉及对映选择性地生产本文公开的δ-内酯和新型中间体的方法。

3. 发明授权

US06229041B1 Preparation of S-aryl-cysteine and its derivatives 有权
标题翻译： S-芳基半胱氨酸及其衍生物的制备
公开(公告)号：US06229041B1
公开(公告)日：2001-05-08
申请号：US09339721
申请日：1999-06-24
申请人： Jack D. Brown , Hiralal N. Khatri , Peter J. Harrington , Dave A. Johnston , Robert J. Topping , Richard R. Dauer , Gary K. Rowe
发明人： Jack D. Brown , Hiralal N. Khatri , Peter J. Harrington , Dave A. Johnston , Robert J. Topping , Richard R. Dauer , Gary K. Rowe
IPC分类号： C07C22716
CPC分类号： C07C319/14 , Y02P20/55 , C07C323/59
摘要： The present invention provides a method for preparing S-aryl cysteine. Specifically, the present invention provides enantioselective method for preparing S-aryl cysteine starting from cystine, cysteine or serine amino acid. The methods of the present invention provides S-aryl cysteine in enantiomeric excess of greater than about 96%.
摘要翻译：本发明提供了制备S-芳基半胱氨酸的方法。具体地，本发明提供了从胱氨酸，半胱氨酸或丝氨酸氨基酸开始制备S-芳基半胱氨酸的对映选择性方法。本发明的方法提供对映体过量的S-芳基半胱氨酸大于约96％。

4. 发明授权

US5808088A Preparation of mibefradil via an acetamide anion 失效
标题翻译：通过乙酰胺阴离子制备米非拉迪
公开(公告)号：US5808088A
公开(公告)日：1998-09-15
申请号：US60151
申请日：1998-04-14
申请人： Peter J. Harrington , Michael P. Fleming
发明人： Peter J. Harrington , Michael P. Fleming
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-1-isopropyl-3,4-dihydro-1H-naphthalen-2-one with the dianion of N-�3-(1H-benzimidazol-2-yl)propyl!-N-methylacetamide 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, (lS,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-2-yl)propyl!-N-methylacetamide, and the acetic acid solvate of 2-�2- {�3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-ol dioxalate, are 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-异丙基-1,2,3,4-四氢化萘-2 - 甲氧基乙酸甲酯包括使6-氟-1-异丙基-3,4-二氢-1H-萘-2-酮与N- [3-（1H-苯并咪唑-2-基）丙基] -N-甲基乙酰胺形成N- [3-（1H-苯并咪唑-2-基）丙基] -2-（6-氟-2-羟基-1-异丙基-1,2,3,4-四氢化萘-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-酮并将2- [2 - {[3-（1H-苯并咪唑-2-基）丙基]甲基氨基}乙基] -6-氟-1-氟丙基-1,2,3,4-四氢化萘 -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米非普利，（1S，2S）-2- [2 - {[3-（1H-苯并咪唑-2-基）丙基]甲基氨基}乙基] -6-氟-2-碘异丙基 -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] -N-甲基乙酰胺，和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-醇二氧杂环己烯，是新的。

5. 发明授权

US07384939B2 Process for preparation of pyridine derivatives of NK-1 receptor antagonist 有权
标题翻译：制备NK-1受体拮抗剂吡啶衍生物的方法
公开(公告)号：US07384939B2
公开(公告)日：2008-06-10
申请号：US11175799
申请日：2005-07-05
申请人： Peter J. Harrington , David A. Johnston , L. Mark Hodges
发明人： Peter J. Harrington , David A. Johnston , L. Mark Hodges
IPC分类号： A61K31/54 , A61K31/497 , A61K31/66 , C07D279/10 , C07D401/00
CPC分类号： C07D213/127 , C07D213/81 , C07D213/82 , C07D213/85 , C07D401/04 , C07D417/04
摘要： The present invention provides a process for preparing a pyridine compound of the formula: wherein R1, R2, R3 and a are those defined herein.
摘要翻译：本发明提供下式的吡啶化合物的制备方法：其中R 1，R 2，R 3和A是定义的这里。

6. 发明授权

US06197976B1 Preparation of ketorolac 有权
标题翻译：酮咯酸的制备
公开(公告)号：US06197976B1
公开(公告)日：2001-03-06
申请号：US09460526
申请日：1999-12-13
申请人： Peter J. Harrington , Hiralal N. Khatri , George C. Schloemer
发明人： Peter J. Harrington , Hiralal N. Khatri , George C. Schloemer
IPC分类号： C07D20952
CPC分类号： C07D487/04
摘要： 5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxamides of the formula where R1 is alkyl and R2 is optionally substituted phenyl, and the method for their preparation and their conversion to ketorolac and its pharmaceutically acceptable salts.
摘要翻译：式R 1的5-苯甲酰基-2,3-二氢-1H-吡咯嗪-1-甲酰胺是烷基，R 2是任选取代的苯基，及其制备方法及其转化为酮咯酸及其药学上可接受的盐。

7. 发明授权

US5567816A Preparation of acyclovir using 1,3 dioxolane 失效
标题翻译：使用1,3-二氧戊环制备无环鸟苷
公开(公告)号：US5567816A
公开(公告)日：1996-10-22
申请号：US426005
申请日：1995-04-27
申请人： George C. Schloemer , Yeun-Kwei Han , Peter J. Harrington
发明人： George C. Schloemer , Yeun-Kwei Han , Peter J. Harrington
IPC分类号： C07D473/00 , C07D473/18
CPC分类号： C07D473/00
摘要： A process for the preparation of acyclovir includes contacting an at least partially silylated guanine or mixture of at least partially silylated guanines with 1,3-dioxolane in the presence of a selective alkylation catalyst selected from the group consisting of trifluoromethanesulfonic acid, trimethylsilyl trifluoromethanesulfonate, and bistrimethylsilyl sulfonate, and hydrolyzing the product thus formed.
摘要翻译：制备无环鸟苷的方法包括在选自烷基化催化剂的存在下使至少部分甲硅烷基化的鸟嘌呤或至少部分甲硅烷化的鸟嘌呤的混合物与1,3-二氧戊环接触，所述选择性烷基化催化剂选自三氟甲磺酸，三氟甲磺酸三甲基甲硅烷基酯和双三甲基甲硅烷基磺酸盐，并水解由此形成的产物。

8. 发明授权

US4845216A Pyrido [2,3,d]pyrimidine derivatives 失效
标题翻译：吡啶并[2,3，d]嘧啶衍生物
公开(公告)号：US4845216A
公开(公告)日：1989-07-04
申请号：US74623
申请日：1987-07-17
申请人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
发明人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , Y02P20/55
摘要： 2,4-Diamino- and 2-amino-4-hydroxy- derivatives of N-(4-[2-(pyrido[2,3-d]pyrimidin-6-yl)alkyl]benzoyl)-L-glutamic acids, and the corresponding 5,6,7,8-tetrahydro compounds are antineoplastic agents. The compounds are prepared by hydrolytic or hydrogenolytic removal of carboxylic acid protecting groups from the correspondingly protected glutamic acid derivatives. A typical embodiment is N-)4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]benzoyl)-L-glutamic acid.
摘要翻译： N-（4- [2-（吡啶并[2,3-d]嘧啶-6-基）烷基]苯甲酰基）-L-谷氨酸的2,4-二氨基 - 和2-氨基-4-羟基 - 相应的5,6,7,8-四氢化合物是抗肿瘤剂。通过水解或氢解除去相应保护的谷氨酸衍生物的羧酸保护基来制备化合物。典型的实施方案是N-）4- [2-（2-氨基-4-羟基-5,6,7,8-四氢吡啶并[2,3-d]嘧啶-6-基）乙基]苯甲酰基）谷氨酸。

9. 发明授权

US06765109B1 Preparation of S-aryl-cysteine and its derivatives 有权
标题翻译： S-芳基半胱氨酸及其衍生物的制备
公开(公告)号：US06765109B1
公开(公告)日：2004-07-20
申请号：US09713134
申请日：2000-11-14
申请人： Jack D. Brown , Hiralal N. Khatri , Peter J. Harrington , Dave A. Johnston , Robert J. Topping , Richard R. Dauer , Gary K. Rowe
发明人： Jack D. Brown , Hiralal N. Khatri , Peter J. Harrington , Dave A. Johnston , Robert J. Topping , Richard R. Dauer , Gary K. Rowe
IPC分类号： C07C22936
CPC分类号： C07C319/14 , C07C323/59
摘要： The present invention provides a method for preparing S-aryl cysteine. Specifically, the present invention provides enantioselective method for preparing S-aryl cysteine starting from cystine, cysteine or serine amino acid. The methods of the present invention provides S-aryl cysteine in enantiomeric excess of greater than about 96%.
摘要翻译：本发明提供了制备S-芳基半胱氨酸的方法。具体地，本发明提供了从胱氨酸，半胱氨酸或丝氨酸氨基酸开始制备S-芳基半胱氨酸的对映选择性方法。本发明的方法提供对映体过量的S-芳基半胱氨酸大于约96％。

10. 发明授权

US5892055A Preparation of mibefradil via an acetamide anion 失效
标题翻译：通过乙酰胺阴离子制备米非拉迪
公开(公告)号：US5892055A
公开(公告)日：1999-04-06
申请号：US106058
申请日：1998-06-26
申请人： Peter J. Harrington
发明人： Peter J. Harrington
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-1-isopropyl-3,4-dihydro-1H-naphthalen-2-one with the dianion of N-�3-(1H-benzimidazol-2-yl)propyl!-N-methylacetamide to form N-�3-(1H-benzirnidazol-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-benzirnidazol-2-yl)propyl!methylarnino}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-2-yl)propyl!-N-methylacetamide, and the acetic acid solvate of 2-�2-{�3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1, 2,3,4-tetrahydronaphthalen-2-ol dioxalate, are 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，甲氧基乙酸甲酯包括使6-氟-1-异丙基-3,4-二氢-1H-萘-2-酮与N- [3-（1H-苯并咪唑-2-基）丙基] -N-甲基乙酰胺的二价阴离子接触到形成N- [3-（1H-苯基咪唑-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，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-苯基咪唑-2-基）丙基]甲基氨基}乙基] -6-氟-1-异丙基-1,2,3,4-四氢化萘-2 - 甲氧基乙酸或甲氧基乙酸的活化衍生物。本发明特别适用于制备米非普利，（1S，2S）-2- [2 - {[3-（1H-苯并咪唑-2-基）丙基]甲基氨基}乙基] -6-氟-2-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] -N-甲基乙酰胺和2- [2 - {[3-（1H-苯并咪唑-2-基）丙基]甲基氨基}乙基的乙酸溶剂化物 ] -6-氟-1-氟丙基-1,2,3,4-四氢萘-2-醇草酸盐是新的。

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