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    PROCESS FOR THE PREPARATION OF ORGANIC COMPOUNDS
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF ORGANIC COMPOUNDS 审中-公开
    制备有机化合物的方法

    公开(公告)号：WO2007085651A1

    公开(公告)日：2007-08-02

    申请号：PCT/EP2007/050816

    申请日：2007-01-29

    申请人： Speedel Experimenta AG ,  HEROLD, Peter ,  STUTZ, Stefan ,  MAH, Robert ,  STOJANOVIC, Aleksandar ,  LYOTHIER, Isabelle ,  BEHNKE, Dirk ,  SPINDLER, Felix ,  BAPPERT, Erhard

    发明人： HEROLD, Peter ,  STUTZ, Stefan ,  MAH, Robert ,  STOJANOVIC, Aleksandar ,  LYOTHIER, Isabelle ,  BEHNKE, Dirk ,  SPINDLER, Felix ,  BAPPERT, Erhard

    IPC分类号： C07D231/56 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D231/56

    摘要： Compounds of the formula I, in which R' 1 and R' 2 represent, independently of one another, H, C 1 -C 8 -alkyl, halogen, polyhalo-C 1 -C 8 -alkoxy, polyhalo-C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxy-C 1 -C 8 -alkyl or C 1 -C 8 -alkoxy-C 1 -C 8 -alkoxy, R' 1 and R' 2 not simultaneously representing H, and R' 3 represents C 1 -C 8 -alkyl and in which the carbon atom to which the R' 3 radical is bonded exhibits either the (R) or (S) configuration, the (R) configuration being preferred, can be obtained in high yields by a stereoselective addition of R' 3 -substituted propionates to RV and R' 2 -substituted unsaturated bicyclic heterocyclyl aldehydes of the formula R-CHO to give corresponding 3-R-3-hydroxy-2-R' 3 -propionates. Conversion of the OH group to a leaving group, subsequently a regioselective elimination to give 3-R-2-R' 3 -propenoates, followed by 1 ) the saponification to give the corresponding 3-R-2-R' 3 -propenoic acids, the enantioselective hydrogenation thereof to give corresponding chiral 3-R-2-R' 3 -propanoic acids and the reduction thereof, or 2) the saponification to give the corresponding 3-R-2-R' 3 -propenoic acids, the reduction thereof to give corresponding 3-R-2-R' 3 -allyl alcohols and the enantioselective hydrogenation thereof, or 3) the reduction to give corresponding 3-R-2-R' 3 -allyl alcohols and the enantioselective hydrogenation thereof, R being

    摘要翻译： 其中R 1'和R“2'的式I化合物彼此独立地表示H，C 1 -C 3烷基， 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 -C 1 - C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基-C R 1'和R“2不同时表示H，R' N 3表示C 1 -C 8 - 烷基，并且其中R'3个基团的碳原子是 （R）或（S）构型可以以高收率通过立体选择性添加R'3 - 取代丙酸酯至RV和R' 式R-CHO的2-取代的不饱和双环杂环基醛，得到相应的3-R-3-羟基-2R'3 - 丙酸酯。 将OH基转化为离去基团，随后进行区域选择性消除，得到3-R-2-R“3 - 丙烯酸酯，然后1）皂化，得到相应的3-R-2 -R'3'-丙烯酸，其对映选择性氢化反应，得到相应的手性3-R-2-R'3'-丙酸及其还原剂，或2） 皂化，得到相应的3-R-2-R“3 - 丙烯酸，将其还原，得到相应的3-R-2-R”3 - 烯丙基 醇和其对映体选择性氢化，或3）还原反应得到相应的3-R-2-R“3 - 烯丙醇及其对映选择性氢化，R为

    PROCESS FOR PREPARING (R OR S)-5-{1-AZIDO-3-[6-METHOXY-5-(3-METHOXY-PROPOXY)-PYRIDIN-3-YLMETHYL]-4-METHYL-PENTYL}-3-ALKYL-DIHYDRO-FURAN-2-ONE
    9.
    发明申请
    PROCESS FOR PREPARING (R OR S)-5-{1-AZIDO-3-[6-METHOXY-5-(3-METHOXY-PROPOXY)-PYRIDIN-3-YLMETHYL]-4-METHYL-PENTYL}-3-ALKYL-DIHYDRO-FURAN-2-ONE 审中-公开
    （R OR S）-5- {1-氨基-3- [6-甲氧基-5-（3-甲氧基 - 丙氧基） - 吡啶-3-基]甲基] -4-甲基戊-3-炔酸的方法 - 二氢 - 呋喃-2-酮

    公开(公告)号：WO2008113835A1

    公开(公告)日：2008-09-25

    申请号：PCT/EP2008/053323

    申请日：2008-03-19

    申请人： SPEEDEL EXPERIMENTA AG ,  HEROLD, Peter ,  MAH, Robert ,  STUTZ, Stefan ,  STOJANOVIC, Aleksandar ,  LYOTHIER, Isabelle ,  BEHNKE, Dirk

    发明人： HEROLD, Peter ,  MAH, Robert ,  STUTZ, Stefan ,  STOJANOVIC, Aleksandar ,  LYOTHIER, Isabelle ,  BEHNKE, Dirk

    IPC分类号： C07D213/69

    CPC分类号： C07D213/69 ,  C07D405/06

    摘要： Compounds of the formula (E), in which R' 3 is isopropyl and R' 4 is C 1 -C 8 -alkyl, and in which the carbon atom to which the R' 3 radical is bonded has either (R) or (S) configuration, preference being given to (R) configuration, are obtainable in high yields A) by a stereoselective addition of isopropyl-substitutedpropionic esters to 6- methoxy-5-(3-methoxypropoxy)pyridine-3-carbaldehyde to give corresponding 2- {hydroxy-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]methyl}-3-methylbutanoic esters, subsequent conversion of the OH group to a leaving group, and a subsequent regioselective elimination to give 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]- meth-(E)-ylidene]-3-methylbutanoic esters, followed by 1) hydrolysis to give the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)- pyridin-3-yl]meth-(E)-ylidene]-3-methylbutanoic acid, the enantioselective hydrogenation thereof to the corresponding chiral 2-[6-methoxy-5-(3-methoxy- propoxy)pyridin-3-ylmethyl]-3-methylbutanoic acid and the reduction thereof,or 2) hydrolysis to the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3- yl]meth-(E)-ylidene]-3-methylbutanoic acid, the reduction thereof to the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]meth-(E)-ylidene]-3- methylbutan-1-ol and the enantioselective hydrogenation thereof, or 3) reduction to the corresponding 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]- meth-(E)-ylidene]-3-methylbutan-1-ol and the enantioselective hydrogenation thereof, or B) by a Sonogashira coupling of 5-bromo-2-methoxy-3-(3-methoxypropoxy)pyridine, SP-P2216_ATE -80- 5-iodo-2-methoxy-3-(3-methoxypropoxy)pyridine or of trifluoromethanesulphonic acid 6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl ester with 2-propyn-1-ol to give 3-[6- methoxy-5-(3-methoxypropoxy)pyridin-3-yl]prop-2-yn-1-ol, followed by addition of an R' 3 -Grignard compound to give 2-[1-[6-methoxy-5-(3-methoxypropoxy)pyridin-3-yl]- meth-(E)-ylidene]-3-methylbutan-1-ol and the enantioselective hydrogenation thereof; substitution of the chiral 2-[6-methoxy-5-(3-methoxy-propoxy)-pyridin-3-ylmethyl]-3- methyl-butan-1-ol resulting from pathways A) or B)to give 5-(2-halomethyl-3-methyl- butyl)-2-methoxy-3-(3-methoxy-propoxy)-pyridine, coupling thereof with a (E)-(R)-5- halo-2-alkyl-pent-4-enoic acid amide, followed by halogenation,hydroxylation lactonizatization and azidation.

    摘要翻译： 式（E）的化合物，其中R'3是异丙基，R'4是C 1 -C 8烷基， （R）或（S）构型，其中R'3'基团所连接的碳原子具有（R）或（S）构型，优选为（R）构型） （3-甲氧基丙氧基）吡啶-3-甲醛立体选择性加成异丙基取代的丙酸酯得到相应的2- {羟基 - [6-甲氧基-5-（3-甲氧基丙氧基） ）吡啶-3-基]甲基} -3-甲基丁酸酯，随后将OH基转化为离去基团，随后进行区域选择性消除，得到2- [1- [6-甲氧基-5-（3-甲氧基丙氧基） 吡啶-3-基] - 甲基 - （E） - 亚基] -3-甲基丁酸酯，然后1）水解，得到相应的2- [1- [6-甲氧基-5-（3-甲氧基丙氧基） 吡啶-3-基]甲基 - （E） - 亚基] -3-甲基丁酸，其对映选择性氢化为相应的手性2- [6-甲氧基-5-（3-甲氧基 - 丙氧基）吡啶-3-基甲基] -3-甲基丁酸及其还原，或2）水解成相应的2- [1- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基]甲基 - （E） - 亚基] -3-甲基丁酸，将其还原为相应的2- [1- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基]甲基 - （E） - 亚基] 3-甲基丁-1-醇及其对映选择性氢化，或3）还原成相应的2- [1- [6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基] - 甲基 - （E） - 亚基] -3-甲基丁-1-醇及其对映选择性氢化，或B）通过5-溴-2-甲氧基-3-（3-甲氧基丙氧基）吡啶的Sonogashira偶联，SP-P2216_ATE -80- -2-甲氧基-3-（3-甲氧基丙氧基）吡啶或三氟甲磺酸6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基酯与2-丙炔-1-醇的混合物，得到3- [6-甲氧基 -5-（3-甲氧基丙氧基）吡啶-3-基]丙-2-炔-1-醇，然后加入R''3 - 标准化合物，得到2- [1- [ 6-甲氧基-5-（3-甲氧基丙氧基）吡啶-3-基] - m （E） - 亚基] -3-甲基丁-1-醇及其对映选择性氢化; 取代由途径A）或B）得到的手性2- [6-甲氧基-5-（3-甲氧基 - 丙氧基） - 吡啶-3-基甲基] -3-甲基 - 丁-1-醇，得到5-（ -2-甲氧基-3-（3-甲氧基 - 丙氧基） - 吡啶，与（E） - （R）-5-卤代-2-烷基 - 戊-4 - 烯酸酰胺，然后卤化，羟基化内酯化和叠氮化。

    PROCESS FOR PREPARING 2-ALKYL-3-HETEROCYCLYL- PROP-2-EN- 1-OL DERIVATIVES
    10.
    发明申请
    PROCESS FOR PREPARING 2-ALKYL-3-HETEROCYCLYL- PROP-2-EN- 1-OL DERIVATIVES 审中-公开
    制备2-烷基-3-环己基 - 丙-2-烯-1-醇衍生物的方法

    公开(公告)号：WO2008055939A3

    公开(公告)日：2008-07-31

    申请号：PCT/EP2007062022

    申请日：2007-11-08

    申请人： SPEEDEL EXPERIMENTA AG ,  HEROLD PETER ,  MAH ROBERT ,  STUTZ STEFAN ,  STOJANOVIC ALEKSANDAR ,  LYOTHIER ISABELLE ,  BEHNKE DIRK

    发明人： HEROLD PETER ,  MAH ROBERT ,  STUTZ STEFAN ,  STOJANOVIC ALEKSANDAR ,  LYOTHIER ISABELLE ,  BEHNKE DIRK

    IPC分类号： C07D231/56

    CPC分类号： C07D231/56

    摘要： Process for preparing a compound of the formula (I) in which Het is a bicyclic unsaturated heterocyclyl bonded to the rest of the molecule via a carbon atom, where the ring not bonded directly to the rest of the molecule is substituted by R 1 and R 2 , R 1 and R 2 are each independently H, C 1 -C 8 -alkyl, halogen, polyhalo-C 1 -C 8 -alkoxy, polyhalo-C 1 -C 8 -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxy-C 1 -C 8 -alkyl, or C 1 -C 8 -alkoxy-C 1 -C 8 -alkoxy, where R 1 and R 2 are not both H, and R 3 is C 1 -C 8 -alkyl, which is characterized in that a) a compound of the formula ( II) in which Het, R 1 and R 2 are each as defined above and X is Br, I, triflate, tosylate or mesylate is reacted with prop-2-yn-1-ol to give a compound of the formula (III) and b) the compound of the formula (III) is reacted with an alkyl-metal compound in which "alkyl" is as defined above for R 3 to give a compound of the formula (I).

    摘要翻译： 制备其中Het是通过碳原子与分子的其余部分键合的双环不饱和杂环基的式（I）化合物的方法，其中不与分子的其余部分键合的环被R 1和R 2，R 1和R 2各自独立地为H，C 1〜 C 8 - 烷基，卤素，多卤代-C 1 -C 8 - 烷氧基，多卤代-C 1 - C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基-C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基 -C 1 -C 8 - 烷氧基，其中R 1和R 2不都是H，R 其特征在于a）式（II）化合物，其中Het，C 1 -C 6烷基，C 1 -C 6烷基， R 1和R 2各自如上所定义，X是Br，I，三氟甲磺酸酯，甲苯磺酸酯或甲磺酸酯与丙-2-炔-1-醇反应，得到 一种化合物 （III）和b）使式（III）的化合物与烷基金属化合物反应，其中“烷基”如上述R 3所定义，得到式（ 一世）。