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20 条记录 (耗时 0.03 秒)

    Enzymatic acylation
    1.
    发明授权
    Enzymatic acylation 失效
    酶酰化

    公开(公告)号：US5902738A

    公开(公告)日：1999-05-11

    申请号：US829280

    申请日：1997-03-31

    申请人： Bernard Orsat ,  Paul Spurr ,  Beat Wirz

    发明人： Bernard Orsat ,  Paul Spurr ,  Beat Wirz

    IPC分类号： C12N9/20 ,  C07C35/18 ,  C12P7/40 ,  C12P7/62 ,  C12P7/64 ,  C12P23/00 ,  C12P7/02 ,  C07C67/02 ,  C12N11/02

    CPC分类号： C12P7/62 ,  C12P23/00

    摘要： A process for making a compound of formula ##STR1## wherein R signifies a C.sub.1-23 -alkyl group or a C.sub.2-23 -alkenyl group containing 1 to 3 double bonds, comprising the steps of (a) reacting a compound of formula ##STR2## with an acylating agent which is in a mixture comprising (i) an organic solvent and (ii) a lipase which is present in suspension, so as to form the compound of formula I; and (b) recovering the compound of formula I is provided for. The process can be used to make (11Z,13Z)-7,10-dihydro-10-hydroxy-retinyl acetate, an starting material for the production of vitamin A acetate.

    摘要翻译： 一种制备下式化合物的方法，其中R表示C1-23-烷基或含1〜3个双键的C2-23链烯基，包括以下步骤：（a）使式的化合物与酰化剂反应， 是在（i）有机溶剂和（ii）存在于悬浮液中的脂肪酶的混合物中，以形成式I化合物; 和（b）回收式I化合物。 该方法可用于制备（11Z，13Z）-7,10-二氢-10-羟基 - 视黄基乙酸酯，一种生产维生素A乙酸酯的原料。

    Process for the preparation of isonicotinic acid derivatives
    3.
    发明授权
    Process for the preparation of isonicotinic acid derivatives 有权
    制备异烟酸衍生物的方法

    公开(公告)号：US07459563B2

    公开(公告)日：2008-12-02

    申请号：US11259880

    申请日：2005-10-27

    申请人： Paul Spurr

    发明人： Paul Spurr

    IPC分类号： C07D213/46

    CPC分类号： C07D213/79

    摘要： The present invention relates to a process for the manufacture of compounds of formula Ia or Ib and pharmaceutically acceptable additional salts thereof, wherein R is lower alkyl. The compounds of formula Ia or Ib are valuable intermediate products for the manufacture of compounds that are pharmaceutically active as adenosine A2a receptor antagonist or metabotropic Glutamate receptor 2 antagonist. Such compounds are important in the regulation of many aspects of cellular metabolism and in the modulation of different central nervous system activities.

    摘要翻译： 本发明涉及制备式Ia或Ib化合物及其药学上可接受的另外的盐的方法，其中R是低级烷基。 式Ia或Ib的化合物是制备作为腺苷A2a受体拮抗剂或代谢型谷氨酸受体2拮抗剂具有药学活性的化合物的有价值的中间产物。 这些化合物在调节细胞代谢的许多方面以及调节不同的中枢神经系统活性中是重要的。

    Process for the preparation of a benzo(a)quinolizione derivative
    5.
    发明授权
    Process for the preparation of a benzo(a)quinolizione derivative 失效
    制备苯并（a）喹嗪酮衍生物的方法

    公开(公告)号：US5578728A

    公开(公告)日：1996-11-26

    申请号：US327159

    申请日：1994-10-21

    申请人： Paul Spurr

    发明人： Paul Spurr

    IPC分类号： A61K31/435 ,  A61P25/20 ,  C07D455/06

    CPC分类号： C07D455/06

    摘要： The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4-oxo-3 -phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.

    摘要翻译： 本发明涉及制备式I的苯并[a]喹嗪酮衍生物的方法，其中式Ⅰ的化合物其中X为卤素且Ph为苯基的式Ⅰbb与一氧化碳在 在（S）-3-乙氧基吡咯烷或低级链烷醇或水的存在下，存在羰基化催化剂; 其中得到10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹嗪-1-羧酸的低级烷基酯，将其转化为相应的游离酸; 并且其中已经获得了10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹嗪-1-羧酸，使其反应性衍生物与（S）-3- 乙氧基吡咯烷。 式I化合物可用于治疗或预防睡眠障碍。

    Process for the preparation of an intermediate of a benzo[a]quinolizinone derivative
    7.
    发明授权
    Process for the preparation of an intermediate of a benzo[a]quinolizinone derivative 失效
    制备苯并[a]喹嗪酮衍生物的中间体的方法

    公开(公告)号：US5561233A

    公开(公告)日：1996-10-01

    申请号：US452793

    申请日：1995-05-30

    申请人： Paul Spurr

    发明人： Paul Spurr

    IPC分类号： A61K31/435 ,  A61P25/20 ,  C07D455/06

    CPC分类号： C07D455/06

    摘要： The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4 -oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.

    摘要翻译： 本发明涉及制备式I的苯并[a]喹嗪酮衍生物的方法，其中式Ⅰ的化合物其中X为卤素且Ph为苯基的式Ⅰbb与一氧化碳在 在（S）-3-乙氧基吡咯烷或低级链烷醇或水的存在下，存在羰基化催化剂; 其中得到10-氯-6,7-二氢-4-氧-3-苯基-4H-苯并[a]喹嗪-1-羧酸的低级烷基酯，将其转化为相应的游离酸; 并且其中已经获得了10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹嗪-1-羧酸，使其反应性衍生物与（S）-3- 乙氧基吡咯烷。 式I化合物可用于治疗或预防睡眠障碍。

    Cyclization process for substituted benzothiazole derivatives
    9.
    发明授权
    Cyclization process for substituted benzothiazole derivatives 失效
    取代苯并噻唑衍生物的环化方法

    公开(公告)号：US07087761B2

    公开(公告)日：2006-08-08

    申请号：US10743613

    申请日：2003-12-22

    申请人： Paul Spurr

    发明人： Paul Spurr

    IPC分类号： C07D277/82

    CPC分类号： C07D277/82

    摘要： The present invention relates to a process for preparation of amino substituted benzothiazole derivatives of formula I wherein R1, R2 and R3 are independently from each other hydrogen, lower alkyl, lower alkoxy or halogen; R4 is hydrogen, lower alkyl, lower alkyloxy, halogen, or is a five or six membered non aromatic heterocyclyl group, unsubstituted or substituted by lower alkyl or an oxo-group, or is —NR5R6, wherein R5 and R5 are independently from each other hydrogen, lower alkyl, —C(O)-lower alkyl, —(CH2)nO-lower alkyl or benzyl, opionally substituted by lower alkyl, or is an five or six membered heteroaryl group; R1 and R2 or R2 and R3 may form together with the corresponding carbon atoms a ring containing —O—CH2—O— or —CH═CH—CH═CH—; R is hydrogen or —C(O)R′; R′ is a five or six membered non aromatic heterocyclyl group, five or six membered heteroaryl group or is aryl, which rings may be substituted by the groups, selected from lower alkyl, halogen-lower alkyl, lower alkoxy, cyano, nitro, —C(O)H, —C(O)OH or by pyrrolidin-1-yl-methyl; n is 1 to 4; or a pharmaceutically acceptable salt thereof, wherein the cyclization is carried out by the treatment of a compound of formula with sulphoxide/HBr/solvent to give the desired products of formula I for R is hydrogen (formula IA) or for R is —C(O)R′ (formula IB)

    摘要翻译： 本发明涉及制备式I的氨基取代的苯并噻唑衍生物的方法，其中R 1，R 2和R 3独立地为 彼此氢，低级烷基，低级烷氧基或卤素; R 4是氢，低级烷基，低级烷氧基，卤素，或是未被取代或被低级烷基或氧代基取代的五或六元非芳族杂环基，或者是-NR

    Process for producing cycloalkenylalkenes
    10.
    发明授权
    Process for producing cycloalkenylalkenes 失效
    生产环己烯酮的方法

    公开(公告)号：US5155255A

    公开(公告)日：1992-10-13

    申请号：US673909

    申请日：1991-03-25

    申请人： Mario Mazzuchelli ,  Milan Soukup ,  Paul Spurr ,  Claude Stritt

    发明人： Mario Mazzuchelli ,  Milan Soukup ,  Paul Spurr ,  Claude Stritt

    IPC分类号： B01J27/08 ,  B01J27/138 ,  C07B61/00 ,  C07C403/12

    CPC分类号： C07C403/12 ,  C07C2101/16

    摘要： A process for the manufacture of certain cycloalkenylalkenes, e.g. vitamin A acetate, comprises dehydrating 1-(5-acetoxy-3-methyl-penta-1,3-dienyl)-2,6,6-trimethyl-cyclo hexanol or 4 aetoxy-1-(5-acetoxy-3-methyl-penta-1,3-dienyl)-2,6,6-trimethyl-cyclohexanol or 1-(9-acetoxy-3,7-dimethyl-4-hydroxy-nona-2,5,7-trienyl)-2,6,6-trimethyl- cyclohexene in the presence of an alkali metal bromide or of manganese bromide or of a hydrate of such a bromide as the catalyst and in an organic solvent.The products are especially suitable as intermediates in carotinoid syntheses.

    摘要翻译： 制备某些环烯基烯烃的方法，例如 维生素A乙酸酯，包括使1-（5-乙酰氧基-3-甲基 - 五-1,3-二烯基）-2,6,6-三甲基 - 环己醇或4-甲氧基-1-（5-乙酰氧基-3-甲基 - 五亚甲基-1,3-二烯基）-2,6,6-三甲基 - 环己烷或1-（9-乙酸基-3,7-二甲基-4-羟基 - 壬-2,5,7-三烯基）-2 ，6,6-三甲基 - 环己烯在碱金属溴化物或溴化锰存在下，或这种溴化物的水合物作为催化剂和有机溶剂中。 该产品特别适合作为中间体的类胡萝卜素合成。