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    NEW PRODUCTION METHOD FOR CEPHALOSPORIN DERIVATIVE
    1.
    发明专利
    NEW PRODUCTION METHOD FOR CEPHALOSPORIN DERIVATIVE 失效

    公开(公告)号：JP2001055392A

    公开(公告)日：2001-02-27

    申请号：JP2000202997

    申请日：2000-07-05

    Applicant: HOFFMANN LA ROCHE

    Inventor： SPURR PAUL ,  TRICKES GEORG

    IPC: C07D501/48 ,  C07B61/00 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/38 ,  C07D501/46 ,  C07D501/52 ,  C07D501/56

    Abstract: PROBLEM TO BE SOLVED: To obtain a cephalosporin derivative useful as an intermediate for pharmaceutically useful cephalosporin in an advantageous process by treating a specific phosphonium salt with a base in toluene and then reacting in the same way with a solution containing a specific aldehyde at a specific temperature and setting the mole ratio of the above reactants in a specific range. SOLUTION: The objective compound of formula IV is obtained by treating a phosphonium salt of formula I (R is H, a lower alkyl or the like substitutable with one or more groups such as carboxy or the like; Ph is phenyl) [e.g. (R, S) (1-cyclopropylmethyl-2-oxo-pyrrolidin-3-yl)-triphenyl-bromophosphonium or the like] with a base in toluene changing into an ylide of formula II and then reacting in the same way a solution containing an aldehyde of formula III (R1 is an amino protecting group; R2 is a carboxy protecting group) in a polar solvent at about -80 to 0 deg.C, and in this case the compound of formula I, the above-mentioned base and the compound of formula III are used in the molar ratio of 1.15:1.1:1.0 to 1.3:1.25:1.0.

    PRODUCTION OF 3-AMINOPYRROLIDINE DERIVATIVE
    2.
    发明专利
    PRODUCTION OF 3-AMINOPYRROLIDINE DERIVATIVE 失效

    公开(公告)号：JP2000053642A

    公开(公告)日：2000-02-22

    申请号：JP489899

    申请日：1999-01-12

    Applicant: HOFFMANN LA ROCHE

    Inventor： KLINKHAMMER UWE ,  SPURR PAUL ,  WANG SHAONING

    IPC: A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/00 ,  A61P31/04 ,  C07D207/14 ,  C07D501/00 ,  C07D501/04 ,  C07D501/56

    Abstract: PROBLEM TO BE SOLVED: To easily obtain in high yield the subject compound useful as a pharmaceutically active substance or intermediate for producing agrochemicals by converting a specific compound to a pyrrolidine derivative in the presence of a specific primary amine followed by reaction of the pyrrolidine derivative under pressure, optionally in a solvent, in the presence of a specific amine. SOLUTION: This compound of formula III or IV (e.g. allyl 3- aminopyrrolidine-1-carboxylate) is obtained by converting a compound of formula I (X is a protected OH) (e.g. methanesulfonic acid 3,4-bis- methanesulfonyloxybutyl ester) to a pyrrolidine derivative of formula II in the presence of a primary amine of the formula R1NH2 (R1 is H, an alkyl or the like)(e.g. benzylamine) followed by reaction of the pyrrolidine derivative pref. under a pressure of 50-80 bar, optionally in a solvent, in the presence of a compound of the formula R2R3NH (R2 and R3 are each H, an alkyl or the like)(e.g. ammonia) pref. at 20-200 deg.C.

    ACYLAYTION BY ENZYME
    3.
    发明专利
    ACYLAYTION BY ENZYME 失效

    公开(公告)号：JPH1036301A

    公开(公告)日：1998-02-10

    申请号：JP9207097

    申请日：1997-04-10

    Applicant: HOFFMANN LA ROCHE

    Inventor： SPURR PAUL ,  ORSAT BERNARD ,  WIRZ BEAT

    IPC: C12N9/20 ,  C07C35/18 ,  C12P7/40 ,  C12P7/62 ,  C12P7/64 ,  C12P23/00

    Abstract: PROBLEM TO BE SOLVED: To obtain a (11Z, 13Z)-7,10-dihydro-10-hyroxyretiny acylate which is useful for production of vitamin A acylate under conditions of easy catalyst separation and high yield by acrylating a specific hydroxyretional compound in the presence of an enzymatic catalyst lipase under specific conditions of the acylation. SOLUTION: This (11Z, 13Z)-7,10-dihydro-10-hyroxyretiny acylate of formula II (R is a 1-23C alkyl or 2-23C alkyl having 1-3 double bonds) is obtained by selectively monoacylating a (11Z, 13Z)-7,10-dihydro-10-hyroxyretinol of formula I with a lipase which is present in a suspension [for example, a suspension of (granulated) diatomaceous earth on which lipase has been fixed, or a suspension of macroporous polyacrylate on which lipase from Candida antarctica has been fixed]. This selective acylation can efficiently prevent formation of undesirable by-products, such as (11Z, 13Z)-7,10-dihydro-10-acetoxyretinyl acetate.

    PRODUCTION OF 2,5-DISUBSTITUTED PYRIDINE
    4.
    发明专利
    PRODUCTION OF 2,5-DISUBSTITUTED PYRIDINE 失效

    公开(公告)号：JPH11116554A

    公开(公告)日：1999-04-27

    申请号：JP23123998

    申请日：1998-08-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： SPURR PAUL

    IPC: A61K31/505 ,  A61K31/535 ,  A61P43/00 ,  C07D213/61 ,  C07D401/14

    Abstract: PROBLEM TO BE SOLVED: To obtain the subject pyridine at a more yield in a smaller number of reaction processes by reacting a specific monoene compound with an acrylic compound, and further reacting with a hydrogen halide. SOLUTION: This objective pyridine expressed by formula III (e.g. 2-chloro-5- isopropylpyridine) is obtained by (A) reacting a compound of the formula: R -CH=CH-R R is a lower alkyl; R is a di(lower alkyl) amino, a 5-membered or 6-membered N-heterocyclic group having a free valence bond on an N-atom} preferably 1-(N-morpholino)prop-1-ene} with an acrylic compound of formula I (X is a halogen) preferably in an anhydrous solvent such as a hydrocarbon halide and in the presence of an acid anhydride, and (B) reacting the resultant compound of formula II with a hydrogen halide (preferably gaseous HBr or HCl, in situ) under an anhydrous condition.

    CYCLIZATION PROCESS FOR SUBSTITUTED BENZOTHIAZOLE DERIVATIVES
    7.
    发明申请
    CYCLIZATION PROCESS FOR SUBSTITUTED BENZOTHIAZOLE DERIVATIVES 审中-公开
    取代的苯并噻唑衍生物的循环过程

    公开(公告)号：WO2004060879A3

    公开(公告)日：2004-11-18

    申请号：PCT/EP0314928

    申请日：2003-12-29

    Applicant: HOFFMANN LA ROCHE

    Inventor： SPURR PAUL

    IPC: C07D277/82 ,  C07D277/84 ,  C07D417/04 ,  C07D417/12

    CPC classification number: C07D277/82

    Abstract: The present invention relates to a process for preparation of amino substituted benzothiazole derivatives of formula (I), wherein R , R and R are independently from each other hydrogen, lower alkyl, lower alkoxy or halogen; R 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 -NR R wherein R and R 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; R and R or R and R 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; and to their pharmaceutically acceptable salts, 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) and for R is -C(O)R' (formula IB).

    Abstract translation: 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彼此独立地为氢，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，卤素或是未取代的或被低级烷基或氧代基取代的或五或六元非芳族杂环基，或者是-NR 5 R 6， 其中R 5和R 6彼此独立地为氢，低级烷基，-C（O） - 低级烷基， - （CH 2）n O-低级烷基或苄基，其被低级烷基经opionally取代，或者是五 或六元杂芳基; R 1和R 2或R 2和R 3可以与相应的碳原子一起形成含有-O-CH 2 -O-或-CH = CH-CH = CH-的环; R是氢或-C（O）R'; R'为五元或六元非芳族杂环基，五元或六元杂芳基或芳基，所述环可以被选自低级烷基，卤素 - 低级烷基，低级烷氧基，氰基，硝基， - C（O）H，-C（O）OH或吡咯烷-1-基 - 甲基; n是1至4; 和其药学上可接受的盐，其中环化通过用亚砜/ HBr /溶剂处理式（III）化合物进行，得到式（I）所需产物，其中R为氢（式IA），R为 - C（O）R'（式IB）。

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