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1. 发明授权

US6127550A Stereospecific preparation of chiral 1-aryl-and 1-heteroaryl-2-substituted ethyl-2-amines 失效
标题翻译：手性1-芳基和1-杂芳基-2-取代的乙基-2-胺的立体特异性制备
公开(公告)号：US6127550A
公开(公告)日：2000-10-03
申请号：US266641
申请日：1999-03-11
申请人： Luc Grondard , Jean-Paul Casimir , Patrick Leon , Michael K. O'Brien , Matthew R. Powers , Daniel Robin
发明人： Luc Grondard , Jean-Paul Casimir , Patrick Leon , Michael K. O'Brien , Matthew R. Powers , Daniel Robin
IPC分类号： C07C303/38 , C07B53/00 , C07C211/27 , C07C213/00 , C07C215/08 , C07C303/00 , C07C303/40 , C07C307/00 , C07C311/16 , C07D203/04 , C07D203/24 , C07D221/18 , C07D333/20 , C07D333/28 , C07F1/02
CPC分类号： C07D333/28 , C07C303/40 , C07D203/24 , C07B2200/07
摘要： This invention is directed to methods for stereospecifically preparing [(1-optionally substituted aryl)- or (1-optionally substituted heteroaryl)]-2-substituted ethyl-2-amines, having chirality at the 2-position, and to intermediates to the substituted ethyl-2-amines.
摘要翻译：本发明涉及立体选择性制备在2-位具有手性的[（1-任选取代的芳基） - 或（1-任选取代的杂芳基）] -2-取代的乙基-2-胺的方法，取代的乙基-2-胺。

2. 发明授权

US5962705A Process for preparing derivatives of the taxoid family 有权
标题翻译：制备紫杉烷类衍生物的方法
公开(公告)号：US5962705A
公开(公告)日：1999-10-05
申请号：US192502
申请日：1998-11-17
申请人： Eric Didier , Gilles Oddon , Denis Pauze , Patrick Leon , Didier Riguet
发明人： Eric Didier , Gilles Oddon , Denis Pauze , Patrick Leon , Didier Riguet
IPC分类号： C07D305/14 , C07D263/06
CPC分类号： C07D305/14 , Y02P20/55
摘要： The present invention relates to a novel process for preparing dialkoxy derivatives of the taxoid family by direct alkylation of the two positions 7 and 10 of deacetylbaccatin or derivatives thereof which are esterified in position 13.
摘要翻译：本发明涉及通过在位置13酯化的脱乙酰基浆果赤霉素或其衍生物的两个位置7和10直接烷基化制备紫杉烷类二烷氧基衍生物的新方法。

3. 发明授权

US5912365A Derivatives of 2-azabicyclo�2.2.1! heptane, their preparation and their application 失效
标题翻译： 2-氮杂双环[2.2.1]庚烷的衍生物及其制备及应用
公开(公告)号：US5912365A
公开(公告)日：1999-06-15
申请号：US914484
申请日：1997-08-19
申请人： Denis Largeau , Patrick Leon
发明人： Denis Largeau , Patrick Leon
IPC分类号： C07D209/02 , C07D209/52 , C07D319/08
CPC分类号： C07D209/02 , C07D209/52
摘要： Novel derivatives of 1R- or 1S-2-azabicyclo�2.2.1!heptane with the general formula (I) or (I'), preparation and their application. ##STR1## In the general formulas (I) and (I'), R represents a hydrogen atom or a group with the formula ##STR2## respectively, in which R.sub.1 represents an alkyl group containing 1-4 carbon atoms and Ar represents an optionally substituted phenyl or a- or b-naphthyl group.
摘要翻译：具有通式（I）或（I'）的1R-或1S-2-氮杂双环[2.2.1]庚烷的新衍生物，其制备及其应用。在通式（I）和（I'）中，R表示氢原子或分别具有式的基团，其中R 1表示含有1-4个碳原子的烷基，Ar表示任选取代的苯基或 - b-萘基。

4. 发明授权

US5637753A Process for the preparation of N-carbonylarylimines useful in the synthesis of therapeutically active taxoids 失效
标题翻译：用于合成治疗活性紫杉烷的N-羰基芳基亚胺的制备方法
公开(公告)号：US5637753A
公开(公告)日：1997-06-10
申请号：US578652
申请日：1996-01-16
申请人： Didier Bernard , Patrick Leon
发明人： Didier Bernard , Patrick Leon
IPC分类号： C07D305/14 , C07B61/00 , C07C249/02 , C07C251/28 , C07C269/06 , C07C271/10 , C07C317/28 , C07C303/00
CPC分类号： C07C269/06 , C07C249/02 , C07C317/28
摘要： A process for the preparation of N-carbonylarylimine of the general formula I: ##STR1## in which Ar represent an aryl radical and R represent a phenyl or t-butoxy radical, by desulphonating the compound of the general formula II. ##STR2## The compounds of formula II are novel when R is t-butoxy.
摘要翻译： PCT No.PCT / FR94 / 00880 Sec。 371日期1996年1月16日 102（e）日期1996年1月16日PCT提交1994年7月13日PCT公布。公开号WO95 / 02576 日期1995年1月26日制备通式I的N-羰基芳基亚胺的方法：其中Ar表示芳基，R表示苯基或叔丁氧基，通过将通式二，当R是叔丁氧基时，式II化合物是新的。

5. 发明授权

US06353096B1 Process of use in converting the 4″(S)-OH functional group of the cladinose unit of an azamacrolide to 4″(R)-NH2 有权
标题翻译：用于将azamacrolide的分裂蛋白单元的4“（S）-OH官能团转化为4”（R）-NH 2的方法
公开(公告)号：US06353096B1
公开(公告)日：2002-03-05
申请号：US09484648
申请日：2000-01-18
申请人： Patrick Leon , Frederic Lhermitte , Ronan Guevel , Denis Pauze , Laurent Garel , Gilles Oddon
发明人： Patrick Leon , Frederic Lhermitte , Ronan Guevel , Denis Pauze , Laurent Garel , Gilles Oddon
IPC分类号： C07H100
CPC分类号： C07H17/08
摘要： The subject-matter of the invention is a process for the stereoselective preparation of a compound of general formula I by stereoselective displacement by a nitrogenous nucleophilic compound of the activated alcohol functional group present at this 4″ position in a corresponding derivative of formula II.
摘要翻译：本发明的主题是通过在相应的式II的衍生物中存在于该“4”位的活性醇官能团的含氮亲核化合物进行立体选择性置换的立体选择性制备通式I化合物的方法。

6. 发明授权

US5808093A L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1!heptane compounds 失效
标题翻译： 2-氮杂双环[2.2.1]庚烷化合物的（1R）非对映异构体的L-酒石酸盐和2-氮杂双环[2.2.1]庚烷化合物的制备
公开(公告)号：US5808093A
公开(公告)日：1998-09-15
申请号：US873285
申请日：1997-06-10
申请人： Michael O'Brien , Patrick Leon , Denis Largeau , Ching Tsuei , Thierry Durand
发明人： Michael O'Brien , Patrick Leon , Denis Largeau , Ching Tsuei , Thierry Durand
IPC分类号： C07D491/18 , C07D209/02 , C07D209/52
CPC分类号： C07D209/52 , C07D209/02 , Y02P20/55
摘要： A compound of formula ##STR1## wherein R is a group of formula ##STR2## R.sub.1 is alkyl; and Ar is optionally substituted aryl.
摘要翻译：式（I）的化合物，其中R是式的基团R1是烷基; 并且Ar是任选取代的芳基。

7. 发明授权

US5707697A Dry paint transfer product having high DOI automotive paint coat 失效
标题翻译：干漆转印产品具有高DOI汽车涂料
公开(公告)号：US5707697A
公开(公告)日：1998-01-13
申请号：US403200
申请日：1995-03-13
申请人： Patrick Leon Spain , Keith Lawson Truog
发明人： Patrick Leon Spain , Keith Lawson Truog
IPC分类号： B05D1/28 , B05D7/00 , B05D7/04 , B29C37/00 , B29C43/20 , B29C45/14 , B29C51/14 , F02D41/22 , B60R13/00
CPC分类号： B05D1/286 , B05D7/04 , B05D7/536 , B05D7/576 , B29C37/0025 , B29C45/14811 , B29C51/14 , B29C2037/0042 , B29C2043/186 , B29C2043/187 , B29C2045/14237 , B29C2795/002 , B29C43/203 , B29K2101/10 , B29K2995/002 , B29K2995/0026 , B29L2009/00 , B29L2009/006 , B29L2031/3005 , B29L2031/722 , Y10T156/1002 , Y10T428/1429 , Y10T428/16 , Y10T428/162 , Y10T428/24843 , Y10T428/24851 , Y10T428/24909 , Y10T428/2982 , Y10T428/3154
摘要： An automotive quality paint coat is laminated to the exterior surface of a molded plastic car body member or panel. In one embodiment, the paint coat includes an exterior clear coat above a color coat. During processing, the clear coat and color coat are each coated on a temporary flexible casting sheet and dried. A high gloss surface is transferred to the clear coat from the casting sheet. The paint coat is then transferred from the casting sheet to a thin, semi-flexible thermoformable plastic backing sheet by dry paint transfer-laminating techniques. The resulting laminate is thermoformed into a complex three-dimensional shape of the car body member or panel. The preformed laminate is then bonded to an underlying plastic substrate material, by injection-cladding techniques, for example, to form the finished article. The paint coat has sufficient elongation to retain exterior automotive appearance and durability properties during thermoforming without deglossing. The backing sheet absorbs defects in the substrate material so the paint coat retains its appearance and durability properties during the injection-cladding step. The finished article comprises a high gloss, defect-free paint coat on the exterior of a molded plastic car body member or panel. Solution-form polyvinylidene fluoride/acrylic paint systems have remarkably high combined gloss and distinctiveness-of-image levels, together with durability properties required for exterior automotive use.
摘要翻译：将汽车优质涂料层合到模制塑料车身部件或面板的外表面上。在一个实施方案中，涂料包括在彩色涂层上方的外部透明涂层。在加工过程中，将透明涂层和彩色涂层各自涂覆在临时柔性铸片上并干燥。高光泽表面从铸片转移到透明涂层。然后通过干漆转印层压技术将涂料从铸片转移到薄的半柔性可热成形的塑料背衬片材上。将所得的层压体热成型为汽车车身件或面板的复杂三维形状。然后通过注射包层技术将预成型的层压板粘合到下面的塑料基材上，以形成成品。涂层具有足够的延伸率，以保持外部汽车外观和热成型时的耐久性，而不会发生变形。背衬片吸收衬底材料中的缺陷，使得涂层在注射包层步骤期间保持其外观和耐久性能。成品包括在模制的塑料车身构件或面板的外部上的高光泽，无缺陷的油漆涂层。溶液型聚偏二氟乙烯/丙烯酸漆系统具有非常高的组合光泽度和独特的图像水平，以及外部汽车使用所需的耐久性。

8. 发明授权

US5684159A L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1!heptane compounds 失效
标题翻译： 2-氮杂双环[2.2.1]庚烷化合物的（1R）非对映异构体的L-酒石酸盐和2-氮杂双环[2.2.1]庚烷化合物的制备
公开(公告)号：US5684159A
公开(公告)日：1997-11-04
申请号：US732024
申请日：1996-10-16
申请人： Michael O'Brien , Patrick Leon , Denis Largeau , Matthew Powers , Thierry Durand
发明人： Michael O'Brien , Patrick Leon , Denis Largeau , Matthew Powers , Thierry Durand
IPC分类号： C07D491/18 , C07D209/02 , C07D209/52
CPC分类号： C07D209/52 , C07D209/02 , Y02P20/55
摘要： A method according to the invention is directed to the preparation of a 2-azadihydroxybicyclo�2.2.1!heptane compound of formula ##STR1## wherein * represents an R chirality, *' represents an S chirality, R is hydrogen or, respectively, a group of formula ##STR2## wherein R.sub.1 is alkyl and Ar is optionally substituted aryl, comprising bishydroxylating a bicyclo�2.2.1!heptene compound of formula ##STR3## wherein *, *' and R are as previously defined, in the presence of about 0.1 mol to about 5 mol % of a metal osmate compound or about 0.06 mol % to about 0.07 mol % osmium tetroxide, and an oxidizing agent capable of regenerating osmium tetroxide. The invention is also directed to the treatment of the (1R) diastereomer of the 2-azadihydroxybicyclo�2.2.1!heptane compound (I) wherein R is a group of formula II with L-tartaric acid, and the L-tartaric acid salt product thereof. Furthermore, the invention is directed to using the (1R) diastereomer of the 2-azadihydroxybicyclo�2.2.1!heptane compound in an acid facilitated acetalizing or ketalizing reaction that results in the protection of the dihydroxy moieties thereof in isopropanol. In addition, the invention is directed to oxidizing a bis O-protected derivative of the (1R) diastereomer of the 2-azadihydroxybicyclo�2.2.1!heptane compound to a corresponding lactam compound in the presence of about 0.01 mol % to about 1 mol % of RuO.sub.2 with about 3 equivalents of an oxidant to form the lactam compound with in an enantiomeric excess ("ee") of greater than or equal to about 95%.
摘要翻译：根据本发明的方法涉及式（I）的化合物（I）的2-氮杂二羟基双环[2.2.1]庚烷化合物，其中*表示R手性，*'表示S 手性，R分别为氢或分别为式（II）的基团，其中R 1为烷基，Ar为任选取代的芳基，其包含双羟基化双酚[2.2.1]庚烯化合物（III）其中*，*'和R如前所定义，在约0.1mol至约5mol％的金属锇酸盐化合物或约0.06mol％至约0.07的存在下 mol％的四氧化锇和能够再生四氧化锇的氧化剂。本发明还涉及其中R是式II的基团与L-酒石酸的2-氮杂二羟基双环[2.2.1]庚烷化合物（I）的（1R）非对映异构体的处理，并且L-酒石酸盐其产品。此外，本发明涉及使用2-氮杂二羟基双环[2.2.1]庚烷化合物的（1R）非对映体在酸促进缩醛或缩酮反应中，其导致保护其在异丙醇中的二羟基部分。此外，本发明涉及在约0.01mol％至约1mol的存在下将2-氮杂二羟基双环[2.2.1]庚烷化合物的（1R）非对映异构体的双O保护的衍生物氧化成相应的内酰胺化合物％的RuO 2与约3当量的氧化剂以形成具有大于或等于约95％的对映体过量（“ee”）的内酰胺化合物。

9. 发明授权

US5662977A Process for manufacturing plastic siding panels with outdoor weatherable embossed surfaces 失效
标题翻译：用于制造具有户外耐候压花表面的塑料壁板的工艺
公开(公告)号：US5662977A
公开(公告)日：1997-09-02
申请号：US628903
申请日：1996-04-08
申请人： Patrick Leon Spain , Keith Lawson Truog
发明人： Patrick Leon Spain , Keith Lawson Truog
IPC分类号： B29C37/00 , B29C59/04 , B32B38/04 , B44C1/17 , B44C1/24 , B44C5/04 , B44F9/02 , A61F13/02
CPC分类号： B32B38/04 , B29C37/0025 , B29C59/04 , B29C59/046 , B44C1/1712 , B44C1/24 , B44C5/0446 , B44F9/02 , B29K2995/0022 , B32B2607/00 , Y10T428/1419 , Y10T428/1457 , Y10T428/1476 , Y10T428/1486 , Y10T428/24355 , Y10T428/24364 , Y10T428/24372 , Y10T428/24479 , Y10T428/2457 , Y10T428/24612 , Y10T428/2486 , Y10T428/24901 , Y10T428/24942
摘要： A process for making plastic siding panels, such as outdoor weatherable vinyl panels with an embossed wood grain pattern, comprises extruding a vinyl sheet, and overlaying on the extruded sheet a flexible carrier sheet having coated thereon (a) matte release layer bonded to the carrier sheet, and (b) decorative coating on the matte release layer facing toward the extruded plastic sheet. An embossing roll applies pressure at elevated temperatures to transfer the decorative coating from the matte release layer and bond it to the extruded sheet, while the embossing roll embosses a three-dimensional impression pattern in the laminate transferred to the extruded sheet. The carrier sheet and its matte release layer are then released from the laminate transferred to the vinyl sheet. The matte release layer transfers a low 75.degree. gloss level, preferably in the range of 8 to 12 gloss units, while enabling free release of the carrier from the embossed low gloss surface at elevated temperatures. In one embodiment, a multi-layer wood grain printed acrylic/polyvinylidene fluoride blended decorative coating is simultaneously transferred to a vinyl extrusion and embossed with a three dimensional wood grain texture. A color coat behind wood grain print coats contains pigment at a level that protects the vinyl substrate from UV deterioration. The matte release layer contains a suspended wax which enhances forming the low gloss surface while improving release of the matte release layer from the transferred laminate. A silicone resin in the matte release coat combines with the wax to further enhance release properties.
摘要翻译：一种用于制造塑料壁板的方法，例如具有压花木纹图案的室外耐候性乙烯基板，包括挤出乙烯基片材，并且在挤出的片材上覆盖其上涂覆有柔性载体片材（a）粘合到载体上的消光层片材，和（b）面向挤出塑料片的无光泽剥离层上的装饰涂层。压花辊在升高的温度下施加压力以将装饰涂层从锍剥离层转移并将其粘合到挤出的片材上，同时压花辊压印转移到挤压片材的层压体中的三维印模图案。然后将载体片和其消光层从转移到乙烯基片上的层压板释放出来。无光泽脱模层转移低75°光泽度，优选在8至12个光泽单位的范围内，同时能够在升高的温度下从浮雕的低光泽表面自由释放载体。在一个实施方案中，多层木纹印刷的丙烯酸/聚偏二氟乙烯混合的装饰涂层同时转移到乙烯基挤出物并用三维木纹纹理压花。木纹印花涂层后面的彩色涂层含有保护乙烯基材料免受紫外线劣化的颜料。无光泽释放层包含悬浮的蜡，其增强了形成低光泽表面，同时改善了从被转移的层压体中消除脱模层。无光泽脱模涂层中的硅树脂与蜡结合以进一步增强剥离性能。

10. 发明授权

US5624933A Process for the preparation of a 6-fluoro-2-halo-quinoline 失效
标题翻译：制备6-氟-2-卤代喹啉的方法
公开(公告)号：US5624933A
公开(公告)日：1997-04-29
申请号：US448404
申请日：1995-06-07
申请人： Herve Garcia , Roland Jacquot , Patrick Leon
发明人： Herve Garcia , Roland Jacquot , Patrick Leon
IPC分类号： C07D215/54 , C07D471/04 , H01N43/42 , C07D215/20 , C07D413/00
CPC分类号： C07D215/54 , C07D471/04
摘要： Method of preparation of 6-fluoro-2-halogen quinoline of general formula (I) wherein R is a hydrogen atom or an alkyl radical and Hal and Hal' are identical or different halogen atoms. The invention is characterized in that a halogenating agent is made to act on hydroxy-1 quinoline of general formula (II) wherein Hal is defined as above and R.sub.1 is defined as R excepting a hydrogen atom, the acid function being optionally released if a 6-fluoro-2-halogen quinoline is to be obtained for which R is a hydrogen atom.
摘要翻译： PCT No.PCT / US94 / 11832 Sec。 371日期：1995年6月7日 102（e）日期1995年6月7日PCT 1994年10月20日PCT PCT。出版物WO94 / 24113 日期：1994年10月27日制备通式（I）的6-氟-2-卤代喹啉的方法，其中R是氢原子或烷基，Hal和Hal'是相同或不同的卤素原子。本发明的特征在于，使卤化剂作用于通式（II）的羟基-1-喹啉，其中Hal如上所定义，R 1定义为R除氢原子外，如果6 - 氟-2-卤代喹啉，其中R是氢原子。

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