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11. 发明公开

EP2013220A1 VERFAHREN ZUR HERSTELLUNG VON CYANOALKYL-, CARBOXYL- UND AMINOCARBONYLGRUPPEN TRAGENDEN BORONSÄUREN UND IHREN DERIVATEN 审中-公开
标题翻译：用于生产氰基烷基，羧基和氨基羰基WEARING硼酸和它们的衍生物
公开(公告)号：EP2013220A1
公开(公告)日：2009-01-14
申请号：EP07711737.2
申请日：2007-03-01
申请人： Archimica GmbH
发明人： MEUDT, Andreas , NERDINGER, Sven , LEHNEMANN, Bernd
IPC分类号： C07F5/02
CPC分类号： C07F5/025
摘要： A process for the manufacture of aminocarbonyl boronic acids of formula (IV) by converting the compounds of formula (III) with a Bronsted base Y(OH)n in a solvent or a solvent mixture, wherein Z represents an optionally substituted arylene, heteroarylene, alkene, heteroalkene, alkylidene, heteroalkylidene, alkenylidene, heteroalkenylidene, alkynylidene, arylalkylene, heteroarylalkylene, arylheteroalkylene, heteroarylheteroalkylene, alkylheteroarylene, heteroalkylheteroarylene, or alkylarylene group; Y represents a metal or ammonium cation of valence n with 0

12. 发明公开

EP1899313A1 VERFAHREN ZUR HERSTELLUNG VON ENANTIOMERENREINEN EPOXIDEN DURCH ADH-REDUKTION VON ALPHA-ABGANGSGRUPPEN-SUBSTITUIERTEN KETONEN UND CYCLISIERUNG 审中-公开
标题翻译：用于生产对映体纯环氧BY ADH还原ALPHA启程组酮和环化
公开(公告)号：EP1899313A1
公开(公告)日：2008-03-19
申请号：EP06754193.8
申请日：2006-06-07
申请人： Archimica GmbH
发明人： MEUDT, Andreas , WISDOM, Richard , BÖHM, Claudius
IPC分类号： C07D303/08
CPC分类号： C07D301/26 , C07D303/08
摘要： The invention relates to a method for producing single enantiomer epoxides by reducing a-leaving group-substituted ketones with (R)- or (S)-selective alcohol dehydrogenases in the presence of a cofactor and optionally a suitable system for regenerating the oxidised cofactor, to produce the corresponding single enantiomer alcohols and subsequently, by means of cyclisation induced by a base, the corresponding single enantiomer epoxides (EQUATION 1 ), wherein in EQUATION 1 LG may stand for F, CI, Br, I, OSO2Ar, OSO2CH3, OSO2R or OP(O)OR2, and R1, R2 and R3, independently of one another, stand for hydrogen, a branched or unbranched, optionally substituted C1-C2O- alkyl radical, symbolise an optionally randomly substituted C3-C10- cycloalkyl or alkenyl radical or a randomly substituted carbo- or heterocyclic aryl radical, or corresponds to a radical from the group CO2R, CONR2, COSR, CS2R, C(NH)NR2, CN, CHaI3, ArO, ArS, RO, RS, CHO, OH, NHR, NR2, Cl, F, Br, I or SiR3.

13. 发明授权

EP1479686B1 Verfahren zur Herstellung von Anilinboronsäuren und ihren Derivaten 有权
标题翻译：一种用于苯胺硼酸和它们的衍生物的制备方法
公开(公告)号：EP1479686B1
公开(公告)日：2006-10-04
申请号：EP04010778.1
申请日：2004-05-06
申请人： Archimica GmbH
发明人： Meudt, Andreas, Dr. , Lehnemann, Bernd, Dr. , Scherer, Stefan, Dr. , Kalinin, Alexei, Dr. , Snieckus, Victor, Dr.
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , Y02P20/55

14. 发明公开

EP2448917A2 VERFAHREN ZUR ENANTIOSELEKTIVEN ADDITION VON ORGANOMETALLISCHEN KOHLENSTOFFNUKLEOPHILEN AN TRIFLUORMETHYLKETONE UND VERWENDUNG DES VERFAHRENS IN DER SYNTHESE VON HIV REVERSE TRANSCRIPTASE INHIBITOREN 审中-公开
标题翻译：方法不对称加成有机金属碳亲核试剂的TO三氟甲基酮及其程序USE IN HIV逆转录酶抑制剂的合成
公开(公告)号：EP2448917A2
公开(公告)日：2012-05-09
申请号：EP10728609.8
申请日：2010-06-25
申请人： Archimica GmbH
发明人： NONNENMACHER, Michael , JUNG, Jörg , MEUDT, Andreas
IPC分类号： C07C243/08 , C07D265/18 , C07C215/70
CPC分类号： C07D265/18 , C07B2200/07 , C07C213/00 , C07C2601/02 , Y02P20/55 , C07C215/70
摘要： The invention relates to a method for producing compounds of the formula A1, wherein the carbon atom to which both the CF3 group and the hydroxy group are bonded is a stereocenter having either the R or the S configuration and wherein R1 and R2 are a C1-C8 alkyl, C3-C8 cycloalkyl, C2-C8 alkenyl, C4-C8 cycloalkenyl, C2-C8 alkynyl, C6-C14 aryl, or C5-C13 heteroaryl group independently of each other, wherein the alkyl, alkenyl, and alkynyl groups are straight-chained or branched and wherein all stated groups are unsubstituted or are mono- or polysubstituted with the same or different substituents selected from the group: halide, NO
2 , SO
3 H, SO
3 Na, SO
3 K, CN, OH, NH
2 , NH-lower alkyl, N-di-lower alkyl, COOH, COO-lower alkyl, lower alkyl, and C3-C6 cycloalkyl, and wherein terminal OH-, NH
2 -, and NH-lower alkyl groups and acidic H atoms are unprotected or are protected with a protective group, wherein a mixture of a zinc(II) salt, an enantiomerically pure or enantiomerically enriched auxiliary of the formula (I), wherein R3 and R4 are C6-C14 aryl, C5-C13 heteroaryl, C1-C8 alkyl, or C2-C8 alkenyl groups or hydrogen independently of each other and R5 and R6 are C6-C14 aryl, C5-C13 heteroaryl, C1-C8 alkyl, C2-C8 alkenyl, or C2-C8 alkynyl groups or hydrogen independently of each other or R5 and R6 together represent a C3-C7 alkylene or C3-C7 alkenylene group and at least one of the centers C1, C2, preferably both, is a stereocenter regardless of the configuration of the other center and has either the R or the S configuration and a second auxiliary, which is selected from the group comprising the alcohols, phenols, mercaptans, amines, carboxylic acids, urea derivatives, or the heterocycles containing nitrogen, oxygen, or sulfur, is reacted with an organic or inorganic base and then is reacted with an organometallic compound R1 -M in which R1 has the meaning specified above and in which M is selected from the group: lithium, sodium, potassium, magnesium halide, magnesium cyanide, magnesium-lower alkyl-alcoholates, and then is reacted with a trifluoromethyl ketone (II), wherein R2 has the meaning stated above.
摘要翻译：本发明涉及一种用于制备式A1的化合物，worin到其中两个CF 3基团和羟基基团所结合的碳原子是具有R或S构型和worin R1和R2是一个C1立体中心 C8烷基，C3-C8环烷基，C2-C8链烯基，C4-C8环烯基，C2-C8炔基，C6-C14芳基，或海誓山盟的C5-C13杂芳基unabhängig，worin烷基，烯基和炔基是直 -chained或支链的并且worin都表示基团是unsubstituiertem或单或与选自相同或不同的取代基取代：卤素，NO 2，SO 3 H，SO 3 Na或-SO 3 K.，CN，OH，NH 2，NH-低级烷基，N 二 - 低级烷基，COOH，COO - 低级烷基，低级烷基，C3-C6环烷基，和worin末端OH，NH 2和NH - 低级烷基基团和酸性氢原子是未保护的或用保护基保护，worin锌（II）盐的混合物，对映体纯或对映体富集的辅助式（I）的，worin R3和R4是C6-C14芳基，C5-C13杂芳基，C1-C8烷基，或C2-C8烯基或氢彼此独立地和R5和R6是C6-C14芳基，C5 -C13杂芳基，C1-C8烷基，C2-C8烯基或C2-C8炔基或氢彼此独立地或R5和R6一起表示的C3-C7亚烷基或C3-C7亚链烯基和中心的至少一个 C1，C2，优选两者，是立体声中心不管其他中心的构型，并且具有R或S构型和第二辅助，它是从包括以下的组的醇，酚，硫醇，cardamines，羧酸选取全部，脲衍生物，或者含有氮，氧或硫的杂环，是在有机或无机碱反应用，然后在有机金属化合物R1 -M其中R 1进行反应与具有上面和其中M所指定的含义是从所选择的组：锂，钠，钾，卤化镁，镁氰化物，镁 - 低级烷基醇化物，然后进行反应与三氟甲基酮（II），worin R2具有如上所述的含义。

15. 发明公开

EP2235028A1 VERFAHREN ZUR HERSTELLUNG VON PHOSPHONSÄUREANHYDRIDEN 有权转让
标题翻译：用于生产膦
公开(公告)号：EP2235028A1
公开(公告)日：2010-10-06
申请号：EP09700501.1
申请日：2009-01-07
申请人： Archimica GmbH
发明人： LEHNEMANN, Bernd, Wilhelm , WISDOM, Richard
IPC分类号： C07F9/38
CPC分类号： C07F9/3895 , Y02P20/127
摘要： The invention relates to a process for preparing optionally organically substituted phosphonic anhydrides directly from the corresponding phosphonic diesters, without the free phosphonic acid being required as an intermediate, according to reaction scheme (I), (II), (III), (IV), (V), (VI) wherein the substituents n, R, R1, R2 and X are each defined as specified in the description.

16. 发明公开

EP1988095A2 Verfarhen zur Herstellung von Aminoaryl- bzw. heteroarylboronsaeuren und ihren Derivaten 有权转让
标题翻译： Verfarhen zur Herstellung von Aminoaryl-bzw 杂芳基硼烷衍生物
公开(公告)号：EP1988095A2
公开(公告)日：2008-11-05
申请号：EP08007689.6
申请日：2008-04-21
申请人： Archimica GmbH
发明人： Kressierer, Christoph J., Dr. , Lehnemann, Bernd Wilhelm, Dr. , Jung, Jörg, Dr.
IPC分类号： C07F5/02
CPC分类号： C07F5/025 , Y02P20/55
摘要： Die Erfindung betrifft ein Verfahren zur Herstellung von Aminoaryl- bzw. -heteroarylboronsäuren und ihren Estern und Salzen, wobei eine gegebenenfalls substituierte Aminoaryl- bzw. -heteroarylverbindung am Stickstoff durch Kondensation mit einer Carbonylverbindung geschützt, dann metalliert und mit einer geeigneten Borverbindung umgesetzt wird, wodurch je nach Aufarbeitung und Entfernung der Schutzgruppe die entsprechende Boronsäure, ihr Anhydrid oder ein Boronsäureester erhalten wird
摘要翻译：氨基芳基或氨基杂芳基 - 硼酸衍生物的制备涉及用保护基羰基转化氨基芳烃或氨基杂芳基化合物以形成保护的氨基芳烃或氨基杂芳烃化合物，随后用硼化合物同时或随后转化以形成受保护的氨基芳基或氨基杂芳基 - 硼化合物（V），并除去保护基以将化合物（V）转化为氨基芳基或氨基杂芳基 - 硼化合物。通式（VI），（VIa）或（VIb）的氨基芳基或氨基杂芳基 - 硼酸衍生物的制备涉及用保护基羰基化合物R'-C（O）-R（A）转化氨基芳烃或氨基杂芳基化合物 “（II）以形成保护的氨基芳烃或氨基杂芳基化合物（III），随后用硼化合物Y 3 -B（Y 1）-Y 2（IV）同时或随后转化以形成受保护的氨基芳基或氨基杂芳基 - 硼化合物（V），除去保护基，将化合物（V）转化为氨基芳基或氨基杂芳基 - 硼化合物（Ⅵ）。芳基：单 - 多环5-20 C-芳基（其中1或2个碳原子任选被O，N或N-R取代）; R：6-12C-芳基，6-12C-芳氧基，杂芳基，杂芳氧基，3-8C-环烷基（全部未取代的单取代或多取代的），1-20C-烷基或1-20C-烷氧基（任选支链和（低级）烷基氨基，二芳基氨基，（低级） - 烷硫基， - 芳硫基，（低级） - 烷氧基羰基或二 - （低级） - 烷基氨基， alkyloxymethylene; X：H，F，Cl，Br或I; Y 1，Y 2，Y 3 H，F，Cl，Br或I，1-20 C-烷氧基（任选支链和任选单或多取代）; Y 1 + Y 2，Y 2 + Y 3，Y 3 + Y 1ring; R'和R“：（低级） - 烷基 - ，芳基 - ，杂芳基 - ，苄基 - ，苄氧基羰基（全部未取代或单取代或多取代）;或R'+ R”+ C：未取代或单取代或多取代的环状部分。新保护的氨基芳基 - 或氨基杂芳基 - 硼化合物（V）包括独立的权利要求。 [图片] [图片]。

17. 发明公开

EP1910276A1 VERFAHREN ZUR HERSTELLUNG VON NITRILEN DURCH ELIMINIERUNGSREAKTIONEN 有权转让
标题翻译：用于生产NITRILES BY消除反应
公开(公告)号：EP1910276A1
公开(公告)日：2008-04-16
申请号：EP06762415.5
申请日：2006-07-05
申请人： Archimica GmbH
发明人： MEUDT, Andreas , NERDINGER, Sven , BÖHM, Claudius
IPC分类号： C07C253/20
CPC分类号： C07C253/20 , C07C255/50 , C07C255/51 , C07C255/54
摘要： Process for preparing nitriles of the formula (II): R-C≡N by reacting N-alkylcarboxamides (RCO-NHR1) or ammonium salts of carboxylic acids (RCOO-NH3R1+) or carboxylic acids in the presence of alkylamines or ammonium salts (RCOOH +NH2R1, RCOOH + NH3R1+), respectively, R being an arbitrarily substituted linear or branched C1-C12- alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl, alkynyl or aryl or heteroaryl radical and R1 being an arbitrary substituted, linear or branched C2-C1 alkyl radical, a C3-C12 cycloalkyl radical or an alkenyl or alkynyl radical, with phosphonic anhydrides in the presence if desired of a base in an organic solvent at a temperature in the range from -30 to 180°C. The phosphonic anhydride used is in particular a 2,4,6-substituted 1,3,5,2,4,6-trioxathiaphosphinane 2,4,6-thoxide of the formula (I).

18. 发明公开

EP1885729A2 VERFAHREN ZUR HERSTELLUNG VON 2-FORMYLFURAN-4-BORONSÄURE DURCH METALLIERUNG VON 4-HALOGENFURFURALACETALEN IN GEGENWART GEEIGNETER BORONSÄUREESTER ODER -ANHYDRIDE 审中-公开
标题翻译：生产由4- HALOGENFURFURALACETALEN的金属化2-甲酰基呋喃-4-硼酸适当硼酸酯或酸酐的存在下
公开(公告)号：EP1885729A2
公开(公告)日：2008-02-13
申请号：EP06742855.7
申请日：2006-05-10
申请人： Archimica GmbH
发明人： MEUDT, Andreas , NERDINGER, Sven , ERBES, Michael , VOGT, William
IPC分类号： C07F5/02
CPC分类号： C07F5/025
摘要： The invention relates to a method for producing furfural-4-boronic acid by the reaction of furfural acetals (I), which are substituted by halogen in position 4, with boronic acid esters or anhydrides (II), by the subsequent metalation of compound (I) and the simultaneous or subsequent reaction with a boronic acid ester or anhydride (II) to form an acetal-protected furfural-4-boronic acid ester. The product is then subjected to an acid hydrolysis, in which the acetal protection group is eliminated, to form furfural-4-boronic acid (III). In said formulae: X represents chlorine, bromine or iodine; R represents a branched, unbranched and/or cyclic, optionally substituted C1-C20 and in particular C1-C8 alkyl group, an optionally substituted C6-C12 aryl group or an optionally substituted C3-C8 cycloalkyl group, whereby the two groups R together can form a ring; R', R'', R''' independently of one another represent acylic or cyclic, branched or unbranched, optionally substituted C1-C20 alkyl groups, or optionally substituted aryl groups, whereby optionally two of the groups R', R'' and R''' together form a ring, or represent additional groups B(OR)3.

19. 发明公开

EP1713763A1 VERFAHREN ZUR HERSTELLUNG VON NITRILEN UND ISONITRILEN DURCH DEHYDRATISIERUNGSREAKTIONEN MIT PROPANPHOSPHONSÄUREANHYDRIDEN 有权转让
标题翻译：用于生产和腈异腈涉及脱水与PROPANPHOSPHONSAEUREANHYDRIDEN
公开(公告)号：EP1713763A1
公开(公告)日：2006-10-25
申请号：EP05700951.6
申请日：2005-01-15
申请人： Archimica GmbH
发明人： MEUDT, Andreas , SCHERER, Stefan , NERDINGER, Sven
IPC分类号： C07C253/20 , C07C253/22 , C07C291/10 , C07C255/50
CPC分类号： C07C253/20 , C07C253/22 , C07C291/10 , C07C255/50
摘要： The invention concerns a method for producing: a) nitriles of formula (II) and; b) isonitriles of formula (III) by reacting: a) carboxylic acid amides (RCO-NH2), ammonium salts of carboxylic acids (RCOO-NH4+) or carboxylic acids in the presence of ammonia or ammonium salts (RCOOH +NH3, RCOOH + NH4+) or; b) formamides (H-CO-NHR) or mixtures of amines with formic acid, with cyclic phosphonic acid anhydrides while eliminating water at a temperature ranging from -30 to +120 °C, in which R represents an arbitrarily substituted linear or branched C1-C8 alkyl radical, a C3-C10 cycloalkyl radical, alkenyl radical, alkynyl radical or an aryl radical or heteroaryl radical. As a cyclic phosphonic acid anhydride, a 2,4,6,-substituted 1,3,5,2,4,6-trioxatriphosphinane-2,4,6-trioxide of formula (I) is used, in which: x = 3, 4 or 5; R', independent of one another, represents open-chain or branched, saturated or unsaturated, straight-chain C1 to C16 alkyl radicals or cyclic C3 to C16 alkyl radicals or aryl or heteroaryl.

20. 发明公开

EP2444390A1 Process for producing Lacosamide 有权
标题翻译： Verfahren zur Herstellung von Lacosamid
公开(公告)号：EP2444390A1
公开(公告)日：2012-04-25
申请号：EP11002024.5
申请日：2011-03-11
申请人： Archimica GmbH
发明人： Wisdom, Richard, Dr. , Jung, Jörg, Dr. , Meudt, Andreas, Dr.
IPC分类号： C07C231/12 , C07C231/14 , C07C237/06 , C07C237/22 , C07C229/22 , C07C271/22
CPC分类号： C07C231/12 , C07B2200/07 , C07C231/14 , C07C231/18 , C07C269/06 , C07C237/22 , C07C271/22
摘要： Summary
The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20 °C.
摘要翻译：发明内容本发明涉及通过（R）-2-乙酰氨基-2-苄基-3-羟基 - 丙酰胺（lacosamide）的甲基化制备（R）-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺丙酰胺（V），其中甲基化在低于20℃的温度下进行。

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