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    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
    7.
    发明申请
    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
    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

    Applicant: ARCHIMICA GMBH ,  NONNENMACHER MICHAEL ,  JUNG JOERG ,  MEUDT ANDREAS

    Inventor： NONNENMACHER MICHAEL ,  JUNG JOERG ,  MEUDT ANDREAS

    IPC: C07C243/08 ,  C07C215/70 ,  C07D265/18

    CPC classification number: C07D265/18 ,  C07B2200/07 ,  C07C213/00 ,  C07C2601/02 ,  Y02P20/55 ,  C07C215/70

    Abstract: 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.

    Abstract translation: 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。

    KRISTALLINE, ENANTIOMERENREINE SALZFORM EINES BETAMIMETIKUMS UND DESSEN VERWENDUNG ALS ARZNEIMITTEL
    9.
    发明申请
    KRISTALLINE, ENANTIOMERENREINE SALZFORM EINES BETAMIMETIKUMS UND DESSEN VERWENDUNG ALS ARZNEIMITTEL 审中-公开
    晶体药物，乙酰胆碱盐及其作为药物的用途

    公开(公告)号：WO2009103479A2

    公开(公告)日：2009-08-27

    申请号：PCT/EP2009/001082

    申请日：2009-02-17

    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  WERTHMANN, Ulrike ,  SANTAGOSTINO, Marco ,  DURAN, Adil

    Inventor： WERTHMANN, Ulrike ,  SANTAGOSTINO, Marco ,  DURAN, Adil

    IPC: C07D265/18 ,  A61P11/00

    CPC classification number: C07D265/18

    Abstract: Die vorliegende Erfindung betrifft ein kristallines, enantiomerenreines Hydrochlorid-Salz von N-(5-{2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino]-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methansulfonamide, bevorzugt von N-(5-{(R)-2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino]-1-hydroxy- ethyl}-2-hydroxy-phenyl)-methansulfonamide und dessen Wirkung als langwirksames Betamimetikum alleine oder in Kombination mit einem oder mehreren, weiteren Wirkstoffen zur Behandlung von Atemwegserkrankungen.

    Abstract translation: 本发明涉及N-（5- {2- [3-（4,4-二乙基-2-氧代-4H-苯并[d] [1 1,3]恶嗪-1-基）-1,1-二甲基 - 丙基氨基] -1-羟基 - 乙基} -2-羟基 - 苯基）-methansulfonamide，优选的N-（5 - {（R）-2- [ 3-（4,4-二乙基-2-氧代-4H-苯并[d] [1,3]恶嗪-1-基）-1,1-二甲基 - 丙基氨基] -1-羟基 - 乙基} -2-羟基 苯基）-methansulfonamide及其作为效果的长效β模拟物单独或与一种或多种其他用于呼吸系统疾病的治疗组合。

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