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    PROCESS FOR THE SEPARATION OF ENANTIOMERS
    1.
    发明申请
    PROCESS FOR THE SEPARATION OF ENANTIOMERS 审中-公开
    分离器的过程

    公开(公告)号：WO2004052883A3

    公开(公告)日：2005-01-13

    申请号：PCT/US0340067

    申请日：2003-12-04

    Applicant: HONEYWELL INT INC

    Inventor： WILKEN JOERG ,  KANSCHIK-CONRADSEN ANDREAS ,  NERENZ FRANK

    IPC: C07B57/00 ,  C07C51/02 ,  C07C51/09 ,  C07C51/41 ,  C07C51/43 ,  C07D405/12

    CPC classification number: C07D405/12 ,  C07B57/00 ,  C07C51/02 ,  C07C51/09 ,  C07C51/412 ,  C07C51/43 ,  C07C59/48

    Abstract: In a process comprising synthesizing pyranes including [R-(R*,R*)]-N-[3-[1 [5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3- yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide the present invention comprises the improvements comprising: (a) providing a racemic mixture of 3-hydroxy- 3-(2-phenylethyl)-hexanoate ethyl acetate by reacting said 1-phenyl-hexan-3-one with ethylbromoacetate under Reformatsky conditions; and (b) separating (R)-3-hydroxy-3- (2-phenylethyl)-hexanoic acid in enantiomeric excess by saponification and reverse resolution of the racemate of step (a) to produce a resolved product. In addition, the present invention comprises a reverse resolution process for separating an enantiomer from a mixture of enantiomers.

    Abstract translation: 在包括合成包括[R-（R *，R *）] - N- [3- [1,5-二羟基-4-羟基-2-氧代-6-（2-苯乙基）-6 - 丙基-2H-吡喃-3-基]丙基]苯基] -5-（三氟甲基）-2-吡啶磺酰胺本发明包括以下改进：（a）提供3-羟基-3-（2- 苯乙基） - 己酸乙酯，通过在Reformatsky条件下使所述1-苯基 - 己-3-酮与溴乙酸乙酯反应; 和（b）通过步骤（a）的外消旋物的皂化和反向拆分来分离对映异构体过量的（R）-3-羟基-3-（2-苯基乙基） - 己酸，得到分离产物。 此外，本发明包括从对映异构体的混合物中分离对映异构体的逆分辨方法。

    METHODS OF PRODUCING PHOSPHITYLATED COMPOUNDS
    2.
    发明申请
    METHODS OF PRODUCING PHOSPHITYLATED COMPOUNDS 审中-公开
    生产磷酸化合物的方法

    公开(公告)号：WO03072586B1

    公开(公告)日：2004-05-13

    申请号：PCT/US0305682

    申请日：2003-02-24

    Applicant: HONEYWELL INT INC

    Inventor： WERNER CHRISTIAN ,  NERENZ FRANC ,  KANSCHIK-CONRADSEN ANDREAS

    IPC: C12N15/09 ,  C07B61/00 ,  C07H19/073 ,  C07H19/10 ,  C07H19/173 ,  C07H19/20 ,  C07B47/00 ,  C07F9/24 ,  C07H21/00

    CPC classification number: C07H19/10 ,  C07H19/20

    Abstract: Provided are methods of producing phosphitylated compounds, including 3'-O­phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of (1) acid-base complexes derived from an amine base of Formula (I) wherein R, R , and R are independently C1-C10 alkyl, C1-C10 cycloalkyl, C1-Cl0 aryl, Cl-C10 aralkyl, Cl-C10 heteroalkyl, or Cl-CIO heteroaryl; (2) acid-base complexes derived from an amine base of Formula (II) wherein R , R , R , R , and are independently hydrogen, C1-C10 alkyl, Cl-C10 cycloalkyl, Cl-C10 aryl, Cl-CIO aralkyl, Cl-CIO heteroalkyl, or C1-C10 heteroaryl, and at least one of R , R , R , R , and R is not hydrogen.; (3) acid-base complexes derived from a diazabicyclo amine base; (4) zwitterionic amine complexes; and (5) combinations of two or more thereof, to produce a phosphitylated compound.

    Abstract translation: 提供了包括3'-O-亚磷酰胺在内的亚磷酸化合物的制备方法，该方法包括在选自以下的亚磷酸化活化剂存在下使含羟基化合物与亚磷酸化剂反应的步骤：（1）衍生自 （I）的胺碱，其中R，R 1和R 2独立地为C 1 -C 10烷基，C 1 -C 10环烷基，C 1 -C 10芳基，C 1 -C 10芳烷基，C 1 -C 10杂烷基或Cl -ClO杂芳基; （2）衍生自其中R 3，R 4，R 5，R 6和R 6独立地为氢，C 1 -C 10烷基，C 1 -C 10烷氧基， C10环烷基，C1-C10芳基，C1-C10芳烷基，C1-C10杂烷基或C1-C10杂芳基，以及R 3，R 4，R 5，R 6和 R 7不是氢。 （3）衍生自二氮杂双环胺碱的酸 - 碱络合物; （4）两性离子胺络合物; 和（5）其两种或更多种的组合以产生亚磷酸化化合物。

    METHODS OF PRODUCING PHOSPHITYLATED COMPOUNDS
    6.
    发明专利
    METHODS OF PRODUCING PHOSPHITYLATED COMPOUNDS 未知

    公开(公告)号：CA2477039A1

    公开(公告)日：2003-09-04

    申请号：CA2477039

    申请日：2003-02-24

    Applicant: HONEYWELL INT INC

    Inventor： KANSCHIK-CONRADSEN ANDREAS ,  NERENZ FRANC ,  WERNER CHRISTIAN

    IPC: C12N15/09 ,  C07B61/00 ,  C07H19/073 ,  C07H19/10 ,  C07H19/173 ,  C07H19/20 ,  C07B47/00 ,  C07H21/00 ,  C07F9/24

    Abstract: Provided are methods of producing phosphitylated compounds, including 3'- O~phosphoramidites, comprising the step of reacting a hydroxyl-containing compound with a phosphitylating agent in the presence of a phosphitylation activator selected from the group consisting of (1) acid-base complexes derived from an amine base of Formula (I) wherein R, R1, and R2 are independently C1-C10 alkyl, C1-C10 cycloalkyl, C1-Cl0 aryl, Cl-C10 aralkyl, Cl- C10 heteroalkyl, or Cl-CIO heteroaryl; (2) acid-base complexes derived from an amine base of Formula (II) wherein R3, R4, R5, R6, and are independently hydrogen, C1-C10 alkyl, Cl-C10 cycloalkyl, Cl-C10 aryl, Cl-CIO aralkyl, Cl-C IO heteroalkyl, or C1-C10 heteroaryl, and at least one of R3, R4, R5, R6, and R 7 is not hydrogen.; (3) acid-base complexes derived from a diazabicyclo amine base; (4) zwitterionic amine complexes; and (5) combinations of two or more thereof, to produce a phosphitylated compound.

    7.
    发明专利
    未知

    公开(公告)号：DE602005007387D1

    公开(公告)日：2008-07-17

    申请号：DE602005007387

    申请日：2005-12-22

    Applicant: HONEYWELL INT INC

    Inventor： WERNER CHRISTIAN ,  KANSCHIK-CONRADSEN ANDREAS ,  FRAUKE PLATZ

    IPC: C07D333/06

    Abstract: A method for the formation of 3-alkylthiophenes or 3-arylthiophenes from 3-halothiophenes. More particularly, improvements on the Kumada coupling reaction for the production of 3-alkylthiophenes or 3-arylthiophenes by reacting a 3-halothiophene with an alkylmagnesiumhalide or arylmagnesiumhalide Grignard reagent in the presence of a catalyst and a 2-methyl tetrahydrofuran solvent. The 2-methyl tetrahydrofuran solvent allows for higher concentrations of the Grignard reagent with minimal or no dithienyl side product generation, achieving higher product yields and at a lower cost than other known methods.

    IMPROVED PROCESS FOR THE KUMADA COUPLING REACTION
    8.
    发明专利
    IMPROVED PROCESS FOR THE KUMADA COUPLING REACTION 未知

    公开(公告)号：CA2594613A1

    公开(公告)日：2006-07-20

    申请号：CA2594613

    申请日：2005-12-22

    Applicant: HONEYWELL INT INC

    Inventor： FRAUKE PLATZ ,  KANSCHIK-CONRADSEN ANDREAS ,  WERNER CHRISTIAN

    IPC: C07D333/06

    Abstract: A method for the formation of 3-alkylthiophenes or 3-arylthiophenes from 3-halothiophenes. More particularly, improvements on the Kumada coupling reaction for the production of 3-alkylthiophenes or 3-arylthiophenes by reacting a 3-halothiophene with an alkylmagnesiumhalide or arylmagnesiumhalide Grignard reagent in the presence of a catalyst and a 2-methyl tetrahydrofuran solvent. The 2-methyl tetrahydrofuran solvent allows for higher concentrations of the Grignard reagent with minimal or no dithienyl side product generation, achieving higher product yields and at a lower cost than other known methods.

    PROCESS FOR ISOMERIZATION OF 2-HALOTHIOPHENE TO-3-HALOTHIOPHENE
    9.
    发明专利
    PROCESS FOR ISOMERIZATION OF 2-HALOTHIOPHENE TO-3-HALOTHIOPHENE 未知

    公开(公告)号：CA2594550A1

    公开(公告)日：2006-07-20

    申请号：CA2594550

    申请日：2005-12-21

    Applicant: HONEYWELL INT INC

    Inventor： WERNER CHRISTIAN ,  KELLERMEIER BERND ,  KANSCHIK-CONRADSEN ANDREAS

    IPC: C07D333/28

    Abstract: An improved process and catalyst system for the isomerization of halothiophenes. More particularly, an improved process for the isomerization of 2-halothiopehenes to 3-halothiophenes by reacting a 2-halothiophene with a catalyst and in the presence of a base. The addition of a base additive to the acidic zeolite catalyst allows the desired isomerization reaction to take place while suppressing side-reactions that result in the decomposition of thiophene rings. The catalyst lifetime is thus increased and the amount of catalyst needed for the reaction is reduced, lowering cost.

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