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    Preparation of N-substituted 2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides
    71.
    发明授权
    Preparation of N-substituted 2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides 有权

    公开(公告)号：US07132569B2

    公开(公告)日：2006-11-07

    申请号：US11254749

    申请日：2005-10-21

    申请人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    发明人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    IPC分类号： C07C233/04 ,  C07C233/05

    CPC分类号： C07D295/185 ,  C07C51/06 ,  C07C57/52 ,  C07C57/76 ,  C07C69/65 ,  C07C231/12 ,  C07C233/09 ,  C07C233/20 ,  C07C235/34 ,  C07C247/12 ,  C07D263/22 ,  C07C237/20

    摘要： From compounds of formula II wherein R1 and R2 are independently of one another H, C1–C6alkyl, C1–C6halogenalkyl, C1–C6alkoxy, C1–C6alkoxy-C1–C6alkyl, or C1–C6alkoxy-C1–C6alkyloxy, R3 is C1–C6alkyl, R4 is C1–C6alkyl, and R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6-alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6-alkyl, C1–C6-dialkylamino-C1–C6-alkyl, C1–C6-alkanoylamido-C1–C6-alkyl, HO(O)C—C1–C6-alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2N—C(O)—C1–C6-alkyl, R6 is C1–C6alkyl, R7 is C1–C6alkyl or C1–C6alkoxy, or R6 and R7 together are tetramethylene, pentamethylene, 3-oxa-1,5-pentylene or —CH2CH2O— substituted, if necessary, with C1–C4-Alkyl, phenyl or benzyl, it is possible—through halolactonization, azidation of the halogen group, ring opening with an amine R5—NH2, and reduction of the azide group to form the amino group—to prepare compounds of formula I wherein R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6alkyl, C1–C6dialkylamino-C1–C6-alkyl, C1–C6alkanoylamido-C1–C6alkyl, HO(O)C—C1–C6alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2—N—C(O)—C1–C6alkyl. If 2(S),7(R)-diastereomer of formula II is used, the 2(S),4(S),5(S),7(S)-diastereomer of formula Ia is obtained in a high degree of purity.

    Process for the preparation of substituted octanoyl amides
    72.
    发明授权
    Process for the preparation of substituted octanoyl amides 失效
    制备取代辛酰基酰胺的方法

    公开(公告)号：US06800769B2

    公开(公告)日：2004-10-05

    申请号：US10333847

    申请日：2003-01-24

    申请人： Stefan Stutz ,  Peter Herold

    发明人： Stefan Stutz ,  Peter Herold

    IPC分类号： C07C24706

    CPC分类号： C07C231/02 ,  C07C247/12 ,  Y02P20/55 ,  C07C237/20

    摘要： Compounds of formula (XII), are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is reacted with an amine to form a carboxamide, the halogen is replaced with azide, if necessary after the introduction of a hydroxy protecting group, the resulting azide is converted to a lactone, the lactone is amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I) or a salt thereof.

    摘要翻译： 式（XII）的化合物在5位上同时卤化并在内酯化下在4位羟化，卤代内酯与胺反应形成羧酰胺，如果需要，在引入羟基后，卤素被叠氮化物置换 将所得的叠氮化物转化为内酯，将内酯酰胺化，然后将叠氮化物转化为胺基，得到式（I）化合物或其盐。

    PREPARATION OF N-SUBSTITUTED 2,7-DIALKYL-4-HYDROXY-5-AMINO-8-ARYL-OCTANOYL AMIDES
    77.
    发明申请
    PREPARATION OF N-SUBSTITUTED 2,7-DIALKYL-4-HYDROXY-5-AMINO-8-ARYL-OCTANOYL AMIDES 有权

    公开(公告)号：US20060041169A1

    公开(公告)日：2006-02-23

    申请号：US11254749

    申请日：2005-10-21

    申请人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    发明人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    IPC分类号： C07C231/12

    CPC分类号： C07D295/185 ,  C07C51/06 ,  C07C57/52 ,  C07C57/76 ,  C07C69/65 ,  C07C231/12 ,  C07C233/09 ,  C07C233/20 ,  C07C235/34 ,  C07C247/12 ,  C07D263/22 ,  C07C237/20

    摘要： From compounds of formula II wherein R1 and R2 are independently of one another H, C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxy, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1-C6alkyloxy, R3 is C1-C6alkyl, and R5 is C1-C6alkyl, C1-C6hydroxyalkyl, C1-C6alkoxy-C1-C6-alkyl, C1-C6alkanoyloxy-C1-C6alkyl, C1-C6aminoalkyl, C1-C6alkylamino-C1-C6-alkyl, C1-C6-dialkylamino-C1-C6-alkyl, C1-C6-alkanoylamido-C1-C6-alkyl, HO(O)C—C1-C6-alkyl, C1-C6alkyl-O—(O)C—C1-C6alkyl, H2N—C(O)—C1-C6alkyl, C1-C6alkyl-HN—C(O)—C1-C6alkyl or (C1-C6alkyl)2N—C(O)—C1-C6-alkyl, R6 is C1-C6alkyl, R7 is C1-C6alkyl or C1-C6alkoxy, or R6 and R7 together are tetramethylene, pentamethylene, 3-oxa-1,5-pentylene or —CH2CH2O— substituted, if necessary, with C1-C4-Alkyl, phenyl or benzyl, it is possible—through halolactonization, azidation of the halogen group, ring opening with an amine R5—NH2, and reduction of the azide group to form the amino group—to prepare compounds of formula I wherein R5 is C1-C6alkyl, C1-C6hydroxyalkyl, C1-C6alkoxy-C1-C6alkyl, C1-C6alkanoyloxy-C1-C6alkyl, C1-C6aminoalkyl, C1-C6alkylamino-C1-C6alkyl, C1-C6dialkylamino-C1-C6alkanoylamido-C1-C6alkyl, HO(O)C—C1-C6alkyl, C1-C6alkyl-O—(O)C—C1-C6alkyl, H2N—C(O)—C1-C6alkyl, C1-C6alkyl-HN—C(O)—C1-C6alkyl or (C1-C6alkyl)2—N—C(O)—C1-C6alkyl. If 2(S),7(R)-diastereomer of formula II is used, the 2(S),4(S),5(S),7(S)-diastereomer of formula Ia is obtained in a high degree of purity.

    Process for the preparation of substituted carboxylic esters
    78.
    发明授权
    Process for the preparation of substituted carboxylic esters 有权
    取代的羧酸酯的制备方法

    公开(公告)号：US07153675B2

    公开(公告)日：2006-12-26

    申请号：US10477739

    申请日：2002-04-26

    申请人： Peter Herold ,  Stefan Stutz

    发明人： Peter Herold ,  Stefan Stutz

    IPC分类号： C12P7/62 ,  C12P7/40 ,  C07C69/02

    CPC分类号： C12P7/62 ,  C12P41/005

    摘要： A process for the preparation of 2(S)-alkyl-5-halogenpent-4-ene carboxylic esters by enzymatic hydrolysis, comprising the steps: a) enzymatic hydrolysis of racemic 2-alkyl-5-halogenpent-4-ene carboxylic esters in aqueous and alkaline medium in the presence of an esterase; b) isolation of 2(S)alkyl-5-halogenpent-4-ene carboxylic esters by extraction with an organic solvent; c) isolation of 2(R)-alkyl-5-halogenpent-4-ene carboxylic acids from the aqueous-alkaline medium; d) Esterification of 2(R)-alkyl-5-halogenpent-4-ene carboxylic acids, e) subsequent racemization to form 2-alkyl-5-halogenpent-4-ene carboxylic esters; and f) return of the racemate obtained in step e) to step a), if necessary together with fresh racemic 2-alkyl-5-halogenpent-4-ene carboxylic esters. The process permits the undesired R-stereoisomers to be converted into the desired 2(S)-alkyl-5-halogenpent-4-ene carboxylic esters to avoid waste product from the synthesis.

    摘要翻译： 通过酶水解制备2（S） - 烷基-5-胡椒基-4-戊烯羧酸酯的方法，包括以下步骤：a）将外消旋的2-烷基-5-胡椒基-4-烯羧酸酯酶 水性和碱性介质在酯酶存在下进行; b）通过用有机溶剂萃取分离2（S）烷基-5-胡椒基-4-烯羧酸酯; c）从水性 - 碱性介质中分离2（R） - 烷基-5-胡椒基-4-戊烯羧酸; d）2（R） - 烷基-5-胡椒基-4-烯羧酸的酯化，e）随后的外消旋化以形成2-烷基-5-胡椒戊-4-烯羧酸酯; 和f）如果必要，将步骤e）中获得的外消旋物质与新鲜外消旋的2-烷基-5-胡椒基-4-烯羧酸酯一起返回到步骤a）。 该方法允许将不期望的R-立体异构体转化为所需的2（S） - 烷基-5-胡椒基-4-烯羧酸酯，以避免合成中的废物。

    Production of N-substituted 2,7-dialkyl-4-hydroxy-5-amino-8-arly-octanoylamides
    79.
    发明授权
    Production of N-substituted 2,7-dialkyl-4-hydroxy-5-amino-8-arly-octanoylamides 失效

    公开(公告)号：US07009078B1

    公开(公告)日：2006-03-07

    申请号：US10048229

    申请日：2000-07-13

    申请人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    发明人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    IPC分类号： C07C233/04 ,  C07C233/05

    CPC分类号： C07D295/185 ,  C07C51/06 ,  C07C57/52 ,  C07C57/76 ,  C07C69/65 ,  C07C231/12 ,  C07C233/09 ,  C07C233/20 ,  C07C235/34 ,  C07C247/12 ,  C07D263/22 ,  C07C237/20

    摘要： From compounds of formula II wherein R1 and R2 are independently of one another H, C1–C6alkyl, C1–C6halogenalkyl, C1–C6alkoxy, C1–C6alkoxy-C1–C6alkyl, or C1–C6alkoxy-C1–C6alkyloxy, R3 is C1–C6alkyl, R4 is C1–C6alkyl, and R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6-alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6-alkyl, C1–C6-dialkylamino-C1–C6-alkyl, C1–C6-alkanoylamido-C1–C6-alkyl, HO(O)C—C1–C6-alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2N—C(O)—C1–C6-alkyl, R6 is C1–C6alkyl, R7 is C1–C6alkyl or C1–C6alkoxy, or R6 and R7 together are tetramethylene, pentamethylene, 3-oxa-1,5-pentylene or —CH2CH2O— substituted, if necessary, with C1–C4-Alkyl, phenyl or benzyl, it is possible—through halolactonization, azidation of the halogen group, ring opening with an amine R5—NH2, and reduction of the azide group to form the amino group—to prepare compounds of formula I wherein R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6alkyl, C1–C6dialkylamino-C1–C6-alkyl, C1–C6alkanoylamido-C1–C6alkyl, HO(O)C—C1–C6alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2—N—C(O)—C1–C6alkyl. If 2(S), 7(R)-diastereomer of formula II is used, the 2(S), 4(S), 5(S), 7(S)-diastereomer of formula Ia is obtained in a high degree of purity.

    Process for the preparation of (R)-2-alkyl-3-phenyl-1-propanols
    80.
    发明授权
    Process for the preparation of (R)-2-alkyl-3-phenyl-1-propanols 失效
    制备（R）-2-烷基-3-苯基-1-丙醇的方法

    公开(公告)号：US06881868B2

    公开(公告)日：2005-04-19

    申请号：US10312992

    申请日：2001-06-26

    申请人： Stefan Stutz ,  Peter Herold ,  Felix Spindler ,  Walter Weissensteiner ,  Thomas Sturm

    发明人： Stefan Stutz ,  Peter Herold ,  Felix Spindler ,  Walter Weissensteiner ,  Thomas Sturm

    IPC分类号： C07C41/20 ,  C07B61/00 ,  C07C29/147 ,  C07C29/17 ,  C07C43/23 ,  C07C69/734 ,  C07C69/736 ,  C07C41/18

    CPC分类号： C07C29/17 ,  C07C29/147 ,  C07C43/23 ,  C07C69/734 ,  C07C33/20 ,  C07C33/30

    摘要： Compounds of formula (I), wherein R1 and R2 are, independently of one another, H,C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxyl, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1-C6alkyloxy, and R3 is C1-C6alkyl, are obtainable in high yiedls by stereoselective addition of R3-substituted propionic acid esters to R1- and R2-substituted benzaldehydes of formula R—CHO to form corresponding 3-R-3-hydroxy-2-R3-propionic acid esters, conversion of the OH group to a leaving group, subsequent regioselective elimination to form 3-R-2-R3-propenic acid esters, and reduction to corresponding 3-R-2-R3-allyl alcohols and their enantioselective hydrogenation, wherein R is (a).

    摘要翻译： 式（I）化合物，其中R 1和R 2各自独立地为H，C 1 -C 3烷基， C 1 -C 6烷基，C 1 -C 6卤代烷基，C 1 -C 6烷氧基，C C 1 -C 6烷氧基-C 1 -C 6烷基或C 1 -C 12 -C 6 -C 6烷氧基-C 1 -C 6烷氧基，R 3是C 1 可以通过立体选择性加成R 3 - 取代的丙酸酯与R 1 - （C 1 -C 6）烷基取代， 和R 2 CHO的R 2取代的苯甲醛形成相应的3-R-3-羟基-2-R 3 - 丙酸酯，OH基团的转化 到离去基团，随后进行区域选择性消除以形成3-R-2-R 3 - 丙酸酯，并还原成相应的3-R-2-R 3 - 烯丙醇及其对映选择性氢化，其中R为（a）。