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1. 发明申请

WO2011032634A1 EFAVIRENZ SALTS, METHOD FOR THE PRODUCTION THEREOF, AND METHOD FOR RELEASE FROM THE SALT 审中-公开
标题翻译：依非韦伦盐，PROCESS FOR THEIR与释放盐
公开(公告)号：WO2011032634A1
公开(公告)日：2011-03-24
申请号：PCT/EP2010005230
申请日：2010-08-26
申请人： ARCHIMICA GMBH , JUNG JOERG , MEUDT ANDREAS , NONNENMACHER MICHAEL
发明人： MEUDT ANDREAS , NONNENMACHER MICHAEL
IPC分类号： C07D265/18
CPC分类号： C07D265/18
摘要： The invention relates to a method for producing compounds according to formula (I), wherein the hydrogen atom bound to the nitrogen is replaced with a metal atom from the series of alkali metals or alkaline-earth metals or with an aluminum atom or a tetraalkylammonium cation and wherein the alkaline-earth metal salts or the aluminum salts of the compound (I) can contain other anions such as fluoride, chloride, bromide, iodide, or sulfate in addition to a deprotonated anion (I).
摘要翻译：中描述了一种制备式（I），其中所述键合在氮氢原子被从系列包括碱金属或碱土金属的金属原子，或由铝原子或四烷基铵阳离子，并且其中所述碱土金属盐或取代的化合物的制备除了化合物（I）的铝盐去质子化（I）还可以含有其它阴离子，例如氟化物，氯化物，溴化物，碘化物，或硫酸根。

2. 发明申请

WO2011000532A3 METHOD FOR THE ENANTIOSELECTIVE ADDITION OF ORGANOMETALLIC CARBON NUCLEOPHILES TO TRIFLUOROMETHYL KETONES AND USE OF THE METHOD IN THE SYNTHESIS OF HIV REVERSE TRANSCRIPTASE INHIBITORS 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：WO2011000532A3
公开(公告)日：2011-05-05
申请号：PCT/EP2010003907
申请日：2010-06-25
申请人： ARCHIMICA GMBH , NONNENMACHER MICHAEL , JUNG JOERG , MEUDT ANDREAS
发明人： NONNENMACHER MICHAEL , JUNG JOERG , MEUDT ANDREAS
IPC分类号： C07C243/08 , C07C215/70 , C07D265/18
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, NO2, SO3H, SO3Na, SO3K, CN, OH, NH2, NH-lower alkyl, N-di-lower alkyl, COOH, COO-lower alkyl, lower alkyl, and C3-C6 cycloalkyl, and wherein terminal OH-, NH2-, 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：中描述了一种方法用于制备式A1的化合物的方法，其中代表键合到两个CF 3基团和羟基基团的碳原子是具有R或S构型，并且其中的手性中心，R1和R2 独立地为C1-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C5-C13杂芳基其中所述烷基，烯基和炔基的直链或支链的并且通过从所述组中选择的相同或不同的取代基，其中所有的所述基团是未取代的或单 - 或多 - 取代的：卤素，NO 2，SO 3 H，SO3Na，-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 - 烷基和C 3 -C 6环烷基，并且其中末端OH，NH 2和NH-低级烷基和酸性氢原子或未被保护与使用锌的混合物的保护基团保护（II）的盐，对映体纯或对映体富集的式（I）的手性辅助其中R3和R4各自独立地是C6-C14芳基，C5-C13杂芳基，C1-C8烷基，C2-C8链烯基，或氢且R5和R6独立地表示C6-C14芳基，C5-C13杂芳基，C1-C8烷基，C2-C8烯基，C2-C8炔基或Wassertoff是或R 5和R 6一起形成一个C3 代表-C 7亚烷基或C 3 -C 7 - 亚烯基，和中心的至少一个C1，C2，优选两者，是独立于其他中心的结构是一个手性中心，R或S构型具有和第二辅助由的组中的醇，酚，硫醇，胺，羧酸，脲衍生物，或含氮，或杂环含硫被选择，其中，所述混合物随后用有机碱或无机碱反应，然后与有机金属化合物R1-M在含氧 R1具有以上给出的含义，并且在从所述组中选择的M是选自：锂，钠，钾，卤化镁，Magnesiumcyanid，镁 - 低级烷基醇化物，然后用三氟甲基酮（II）其中R 2具有上述含义，实现。

3. 发明申请

WO2008064817A2 METHOD FOR THE STEREOSELECTIVE SYNTHESIS OF CHIRAL EPOXIDES BY ADH REDUCTION OF KETONES SUBSTITUTED WITH ALPHA STARTING GROUPS AND CYCLISATION 审中-公开
标题翻译：一种通过ADH减持ALPHA启程组酮和环化手性环氧化物立体选择性合成
公开(公告)号：WO2008064817A2
公开(公告)日：2008-06-05
申请号：PCT/EP2007010125
申请日：2007-11-22
申请人： ARCHIMICA GMBH , MEUDT ANDREAS , WISDOM RICHARD A
发明人： MEUDT ANDREAS , WISDOM RICHARD A
IPC分类号： C07D303/08
CPC分类号： C07D303/08
摘要： The invention relates to a method for producing chiral epoxides by reducing ketones substituted with a-starting groups with cell-free (R)- or (S)-selective alcohol dehydrogenases in the presence of a cofactor, and optionally a suitable system for the regeneration of the oxidised cofactor to form the chiral alcohols, and subsequent base-induced cyclisation to form the chiral epoxides (EQUATION 1) wherein LG can represent F, Cl, Br, I, OSO 2 Ar, OSO 2 R 4 or OP(O)OR 4 R 5 and R 1 , R 2 and R 3 independently represent hydrogen, a branched or unbranched, optionally substituted C 1 -C 20 alkyl radical, an optionally substituted C 3 -C 10 cycloalkyl or alkenyl radical or an optionally substituted carbocyclic or heterocyclic aryl radical or a radical from the group consisting of CO 2 R 4 , CONR 4 R 5 , COSR 4 , CS 2 R 4 , C(NH)NR 4 R 5 , CN, CHaI 3 , OAr, SAr, OR 4 , SR 4 , CHO, OH, NR 4 R 5 , Cl, F, Br, I or SiR 4 R 5 R 6 , where R 4 , R 5 and R 6 independently represent hydrogen, a branched or unbranched, optionally substituted C 1 -C 20 alkyl radical, an optionally substituted C 3 -C 10 cycloalkyl or alkenyl radical or a substituted carbocylic or heterocyclic aryl radical, the intermediately formed chiral alcohol Il not being isolated.
摘要翻译：一种用于生产手性环氧化物，通过还原处理的离去基团 - 取代的酮与（R）无细胞 - 或（S） - 选择性醇中的辅因子的存在下脱氢酶，和任选的合适的系统，以再生氧化的辅因子的手性醇与随后的碱诱导的环化手性环氧化物（式1）其中LG是F，Cl，溴，I，OSO _{2 的Ar，OSO _{2 - [R _{4 或 OP（O）OR _{4 - [R _{5 是且R _{1 ，R _{2 和R _{3 独立地表示氢，分支或未分支的，任选取代的C 1 -C 20烷基，任选取代的C 3 -C 18烷基， -C _{10 的环烷基，或烯基，或任选取代的碳环或杂环芳基或基团选自CO _{2 - [R _{4 ，CONR _{4 R _{5 ，COSR _{4 ，CS _{2 - [R _{4 ，C（NH）NR _{4 - [R _{5 ，CN，柴_{3 ，桨，SAR，OR _{4 ，SR _{4 ，CHO，OH，NR _{4 - [R _{5 ，为Cl，F，Br，I或SIR _{4 - [R _{5 - [R _{图6是，其中R _{4 ，R _{5 和R _{6 独立地是氢，支链或无支链，任选取代的C _{1 -C _{20 烷基，任选取代的C _{3 -C _{10 象征环烷基，链烯基或取代的碳环或杂环芳基，和手性中间形成的酒精不是孤立的。}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}

4. 发明申请

WO2006097221A3 METHOD FOR PRODUCING ALKYL-SUBSTITUTED AROMATIC AND HETEROAROMATIC COMPOUNDS BY CROSS-COUPLING ALKYL BORONIC ACIDS WITH ARYL- OR HETEROARYL-HALOGENIDES OR SULFONATES UNDER PD CATALYSIS IN THE PRESENCE OF A LIGAND 审中-公开
标题翻译：生产由与芳基烷基硼酸或杂芳基或磺酸盐交叉耦合烷基取代的芳族化合物和杂芳族化合物UNDER PD CATALYSIS在配体的存在下
公开(公告)号：WO2006097221A3
公开(公告)日：2007-01-04
申请号：PCT/EP2006002061
申请日：2006-03-07
申请人： ARCHIMICA GMBH , SCHERER STEFAN , MEUDT ANDREAS , NERDINGER SVEN , LEHNEMANN BERND , JAGUSCH THOMAS , SNIECKUS VICTOR
发明人： SCHERER STEFAN , MEUDT ANDREAS , NERDINGER SVEN , LEHNEMANN BERND , JAGUSCH THOMAS , SNIECKUS VICTOR
IPC分类号： C07B37/04 , C07C17/26 , C07C25/13 , C07C67/30 , C07C69/76 , C07F5/02
CPC分类号： C07C1/321 , C07B37/04 , C07C17/263 , C07C67/343 , C07C2531/24 , C07D213/30 , C07C15/02 , C07C22/08 , C07C69/76
摘要： The invention relates to a method for producing alkyl-substituted aromatic and heteroaromatic compounds (III) by cross-coupling alkyl boronic acids (II) with aryl- or heteroaryl-halogenides or with aryl- or heteroaryl-sulfonates (I) in the presence of a catalyst and of a Brønsted base in a solvent or solvent mixture, in which: Hal represents chlorine, bromine, iodine, trifluoromethanesulfonate, nonafluorotrimethyl methane sulfonate, methane sulfonate, 4-toluolsulfonate, benzene sulfonate, 2- naphthalene sulfonate, 3-nitrobenzene sulfonate, 4-nitrobenzene sulfonate, 4-chlorobenzene sulfonate or 2,4,6-triisopropylbenzene sulfonate; X 1-5 , independent of one another, represent carbon, X i R i represents nitrogen, or each two adjacent X i R i 's bound via a formal double bond represent, together, O (furane), S (thiophene), NH or NR i (pyrrole); radicals R 1-5 represent substituents from the group consisting of {hydrogen, methyl, primary, secondary or tertiary, cyclic or acyclic alkyl radicals having 2 to 20 C atoms, in which optionally one or more hydrogen atoms are substituted by fluoride or chlorine or bromine, e.g. CF 3 , substituted cyclic or acyclic alkyl groups, hydroxy, alkoxy, amino, alkylamino, dialkylamino, arylamino, diarylamino, alkylarylamino, phenyl, substituted phenyl, heteroaryl, substituted heteroaryl, thio, alkylthio, arylthio, diarylphosphino, dialkylphosphino, alkylarylphosphino, optionally substituted aminocarbonyl, CO 2
摘要翻译：一种用于通过交叉耦合烷基硼酸（II）与芳基或杂芳基卤化物或芳基或Heteroarylsulfonaten（I）（III）制备烷基取代的芳族化合物和杂芳族化合物，在催化剂和布朗斯台德碱在溶剂或溶剂混合物的存在下，其中Hal是过程氯，溴，碘，三氟甲磺酸酯，Nonafluortrimethylmethansulfonat，甲磺酸盐，4-甲苯磺酸盐，苯磺酸盐，2- Naphtalensulfonat，3-硝基苯磺酸，4-硝基苯磺酸酯，4-氯苯或2,4,6-三异丙基，X _{1-5 独立地是碳，X _{I - [R _{I 是氮，或在每种情况下两个相邻的通过正式的双键X _{连接的I - [R _{I 一起是O（呋喃），S（噻吩），NH或NR _{I （吡咯）被提供时，基团R _{1-5 选自{氢，甲基，初级的取代基，仲重或2至20个碳原子具有叔，环状或非环状的烷基基团，其中任选的一个或多个氢原子被氟或氯或溴，例如取代 CF _{3 ，取代的环状或无环烷基，羟基，烷氧基，氨基，烷基氨基，二烷基氨基，芳基氨基，二芳基氨基，烷基芳基氨基，苯基，取代的苯基，杂芳基，取代的杂芳基，硫基，烷硫基，芳硫基，二芳基膦， dialkylphosphino，Alkylarylphosphino，任选取代的氨基羰基，CO ₂}}}}}}}}

5. 发明申请

WO2006122683A3 METHOD FOR PRODUCING 2-FORMYLFURAN-4-BORONIC ACID 审中-公开
标题翻译：用于生产2-甲酰基呋喃-4-硼酸
公开(公告)号：WO2006122683A3
公开(公告)日：2007-05-03
申请号：PCT/EP2006004369
申请日：2006-05-10
申请人： ARCHIMICA GMBH , MEUDT ANDREAS , NERDINGER SVEN , ERBES MICHAEL , VOGT WILLIAM
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 C 1 -C 20 and in particular C 1 -C 8 alkyl group, an optionally substituted C 6 -C 12 aryl group or an optionally substituted C 3 -C 8 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 C 1 -C 20 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 .
摘要翻译：由糠醛缩醛（I），它是卤素取代的在与硼酸酯或酸酐（II）的4位，与硼酸酯反应通过用同时或随后的反应化合物（I）的金属化用于生产糠醛-4-硼酸的方法，或酸酐（Ⅱ）化合物进行缩醛保护糠醛-4-硼酸酯和随后的酸性水解，用乙缩醛的裂解，糠醛-4-硼酸（III）。其中X是氯，溴或碘，R是支链，无支链和/或环状的，任选取代的C _{1 -C _{20 ，特别是C _{1 < / SUB> -C _{8 烷基，任选取代的C _{6 -C _{12 的芳基或任选取代的C _{3 < / SUB> -C _{8 环烷基，其中两个基团R可以一起形成环; R1，R”，R ''”各自独立地表示非环状或环状的，支链或无支链，任选取代的C _{1 -C _{20 的烷基，或任选取代的芳基，任选两个基团R”，R“和R ''”的一起形成环，或为其它基团B（OR）_{3 是。}}}}}}}}}}}

6. 发明申请

WO2005080403A3 CHEMICAL PROCESS 审中-公开
标题翻译：化学工艺
公开(公告)号：WO2005080403A3
公开(公告)日：2005-11-24
申请号：PCT/GB2005000567
申请日：2005-02-17
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , BUTLIN MARGARET ANNE , BUTLIN ROGER JOHN , HOGAN PHILIP JOHN , MEUDT ANDREAS
发明人： BUTLIN MARGARET ANNE , BUTLIN ROGER JOHN , HOGAN PHILIP JOHN , MEUDT ANDREAS
IPC分类号： C07D401/14 , C07F5/02
CPC分类号： C07D401/14 , C07D413/14 , C07F5/025 , Y02P20/55
摘要： Process for preparing compounds of Formula (I); and (IV); are described.
摘要翻译：制备式（I）化合物的方法; 和（IV）; 被描述。

7. 发明申请

WO03033503A2 METHOD FOR PRODUCING, VIA ORGANOMETALLIC COMPOUNDS, ORGANIC INTERMEDIATE PRODUCTS 审中-公开
标题翻译：方法的有机中间体产品ORGANOMETALLIC生产
公开(公告)号：WO03033503A2
公开(公告)日：2003-04-24
申请号：PCT/EP0211042
申请日：2002-10-02
申请人： CLARIANT GMBH , MEUDT ANDREAS
发明人： MEUDT ANDREAS
IPC分类号： C07C45/46 , C07C51/15 , C07D333/16 , C07F1/02 , C07F5/02 , C07F5/04
CPC分类号： C07F5/025 , C07C45/46 , C07C51/15 , C07D333/16 , C07F1/02 , C07C49/807 , C07C63/06
摘要： The invention concerns a method for producing aryllithium compounds of formulas (IV) and (VI) by reacting halogenated compounds (I) with metal lithium, to obtain a lithium compound of formula (II), then in subsequently reacting (II) with aromatic compounds of formula (III) and/or (V) with deprotonation and formation of aromatic products of lithium (IV) and/or (VI) (equation I). Step 1: producing the base; step 2: deprotonation of the substrate; (equation I), formulae wherein R represents methyl, primary, secondary or tertiary alkyl radical containing 2 to 12 carbon atoms, alkyl substituted by a radical from the group (phenyl, substituted phenyl, aryl, heteroaryl, alkoxy, dialkyamino, alkylthio) or substituted or unsubstituted cycloalkyl containing 3 to 8 carbon atoms; Hal = fluorine, chlorine, bromine or iodine; X1-4 independently represent a carbon, the group X1-4R1-4 may represent a nitrogen, or two neighbouring X1-4R1-4 may together represent O, S, NH of NR', wherein R' represents C1-C5 alkyl, SO2-p-tolyl or benzoyl; the radicals R1-4 and the radical Z represent substituents of the group {hydrogen, methyl, substituted cyclic or acyclic primary, secondary or tertiary alkyl radicals containing 2 to 12 carbon atoms, substituted cyclic or acyclic alkyl groups, alkoxy, dialkylamino, arylamino, diarylamino, phenyl, substituted phenyl, alkylthio, diarylphosphino, dialkylphosphino, dialkyl or diarylaminocarbonyl, monoalkyl- or monoarylaminocarbonyl, CO2-, hydroxyalkyl, alkoxyalkyl, fluorine, chlorine, CN or heteroaryl}, the two neighbouring R1-4 radicals capable of forming together an aromatic or aliphatic cycle.
摘要翻译：一种通过卤素化合物（I）的反应与锂金属制备式（IV）和（VI）的芳基锂化合物，以式的锂化合物（II）和另外的反应工艺（II）与式（III）和/或芳族化合物（ V）下脱质子化和形成锂芳烃（IV）和/或（VI）（式I）。步骤1：制备基体的; 步骤2：在基板的去质子化，其中R选自下组的取代的甲基，伯，仲或叔烷基基团具有2至12个碳原子，通过自由基{苯基，取代苯基，芳基，杂芳基，烷氧基，二烷基氨基，烷硫基}烷基，取代或未取代的碳原子数3〜8取代的环烷基，表示哈尔=氟，氯，溴或碘，X1-4各自独立地是碳，分组X1-4 R1-4可以指氮或两个相邻基团 X1-4 R1-4可以 '其中R' 一起代表O，S，NH或NR为C1-C5烷基，SO 2 - 苯基，SO 2 - 对甲苯基或苯甲酰基; 基团R 1-4与基团Z是选自{氢，甲基，伯，仲或叔的，环状的或无环的2至12个碳原子，取代的环状或无环烷基，烷氧基，二烷基氨基，烷基氨基的烷基的基团的取代基，芳基氨基，二芳基氨基，苯基，取代的苯基，烷硫基，二芳基膦，dialkylphosphino，二烷基或diarylaminocarbonyl，单烷基或Monoarylaminocarbonyl，CO 2，羟烷基，烷氧基烷基，氟或氯，CN，或杂芳基}，其中在每种情况下，两个相邻的基团一起R1-4 可以形成芳香族或脂肪族环。

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