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12 条记录 (耗时 0.011 秒)

    Process for the manufacture of a product of the thiazolo [3,4,5-de] [4,1]benzothiazepine type
    6.
    发明授权
    Process for the manufacture of a product of the thiazolo [3,4,5-de] [4,1]benzothiazepine type 失效
    制备噻唑并[3,4,5-de] [4,1]苯并硫氮杂类产物的方法

    公开(公告)号：US07179909B2

    公开(公告)日：2007-02-20

    申请号：US11005224

    申请日：2004-12-06

    申请人： Stephane Mutti ,  Joel Malpart ,  Michel Lavigne ,  Michel Cheve

    发明人： Stephane Mutti ,  Joel Malpart ,  Michel Lavigne ,  Michel Cheve

    IPC分类号： C07D513/06

    CPC分类号： C07C271/28

    摘要： Novel processes for the preparation of a compound of the thiazolo[3,4,5-de] [4,1]benzothiazepine type and in particular of 2-imino-9-trifluoromethyl-4,5-dihydro-2H,7H-thiazolo[3,4,5-de] [4,1]benzothiazepine 6,6-dioxide methanesulfonate and (R,S)-2-imino-9-trifluoromethyl-4,5-dihydro-2H,7H-thiazolo[3,4,5-de] [4,1]benzothiazepine 6-oxide and its enantiomers and their pharmaceutically acceptable salts.

    摘要翻译： 制备噻唑并[3,4,5-de] [4,1]苯并硫氮杂类化合物，特别是2-亚氨基-9-三氟甲基-4,5-二氢-2H- 7H-噻唑的化合物的新方法 [3,4,5-de] [4,1]苯并硫氮杂六甲醚甲磺酸盐和（R，S）-2-亚氨基-9-三氟甲基-4,5-二氢-2H- 7H-噻唑并[ 4,5-de] [4,1]苯并硫氮杂_6-氧化物及其对映体及其药学上可接受的盐。

    METHOD FOR PREPARING COMBRETASTATIN
    7.
    发明申请
    METHOD FOR PREPARING COMBRETASTATIN 审中-公开
    制备化合物的方法

    公开(公告)号：US20110124899A1

    公开(公告)日：2011-05-26

    申请号：US12869997

    申请日：2010-08-27

    申请人： Marc FREDERIC ,  Sylviane LUTZ ,  Joel MALPART ,  Philippe MASSON ,  Stephane MUTTI

    发明人： Marc FREDERIC ,  Sylviane LUTZ ,  Joel MALPART ,  Philippe MASSON ,  Stephane MUTTI

    IPC分类号： C07F9/6571 ,  C07C231/00 ,  C07B57/00

    CPC分类号： C07C217/84 ,  C07B2200/07 ,  C07C231/18 ,  C07C237/04 ,  Y02P20/55

    摘要： The Invention relates to a method for preparing a combretastatin (A): formula (I) in the form of a base or of an addition salt with an acid, which comprises coupling, in the presence of a base and of T3P, the salt of the (Z)-amino compound of formula (II) with a doubly protected L-serine derivative of formula (III) in which PG denotes a group protecting the amine function, so as to obtain the compound of formula (Z)-(Ib): formula (IV), then deprotecting and opening the ring of (Z)-(Ib) in the presence of an acid, so as to obtain the combretastatin (A) in the form of a salt; and, optionally, adding a base, so as to obtain the combretastatin (A) in the form of a base, the salt of the (Z)-amino compound having been obtained by enrichment of the salt of the amino compound of formula (V) in (Z) isomer.

    摘要翻译： 本发明涉及一种制备考布他汀（A）的方法：式（I）：碱的形式或与酸形成的加成盐，其包括在碱和T3P的存在下，将 式（II）的（Z） - 氨基化合物与双重保护的式（III）的L-丝氨酸衍生物，其中PG表示保护胺官能团的基团，以获得式（Z） - （Ib ）：式（Ⅳ），然后在酸存在下使（Z） - （Ib）的环脱保护和开环，得到盐形式的考布他汀（A）; （Z） - 氨基化合物的盐，通过将式（V）的氨基化合物的盐富集而得到的（Z） - 氨基化合物的盐， ）（Z）异构体。

    Novel process for preparing 3-fluoroquinolines
    9.
    发明申请
    Novel process for preparing 3-fluoroquinolines 失效
    制备3-氟喹啉的新方法

    公开(公告)号：US20050182259A1

    公开(公告)日：2005-08-18

    申请号：US10985533

    申请日：2004-11-10

    申请人： Youssef El-Ahmad ,  Jean-Pierre Leconte ,  Joel Malpart ,  Serge Mignani ,  Stephane Mutti ,  Michel Tabart

    发明人： Youssef El-Ahmad ,  Jean-Pierre Leconte ,  Joel Malpart ,  Serge Mignani ,  Stephane Mutti ,  Michel Tabart

    IPC分类号： C07D215/18 ,  C07D215/38 ,  C07D215/12

    CPC分类号： C07D215/38 ,  C07D215/18 ,  Y02P20/55

    摘要： The invention relates to a novel preparation of 3-fluoroquinolines of formula (I) in which R1, R2, R3 and R4 represent: a) a fluorine; b) an alkyl optionally substituted with one to three fluorines, with OR5 in which R5 is an alkyl, a hydrogen or a hydroxyl-protecting group, or with NR′R″ in which R′ and R″ represent an alkyl, a hydrogen or an amino-protecting group; c) OR6 in which R6 represents a hydrogen, a phenol-protecting group or an alkyl, optionally substituted with a fluorine, with OR5 or with NR′R″ as defined above; d) NR′1R″1 in which R′1 and R″1 have the values of R′ et R″ or represent an alkyl substituted with a fluorine, with OR5 or NR′R″ as defined above; e) CO2Ra, in which Ra represents hydrogen, alkyl or a carboxyl-protecting group, and also novel intermediate compounds. The quinolines of formula (I) are intermediates useful in the preparation of compounds having antibacterial activity, described in particular in applications WO 02/40474 or WO 02/72572.

    摘要翻译： 本发明涉及式（I）的3-氟喹啉的新型制备方法，其中R 1，R 2，R 3和R 3， 代表：a）氟; b）任选被一至三个氟取代的烷基，其中R 5是烷基，氢或羟基保护基或NR' 其中R'和R“表示烷基，氢或氨基保护基的”R“ c）OR 6其中R 6表示氢，苯酚保护基或任选被氟取代的烷基，OR 5或N >或如上定义的NR'R“ d）NR'1 R“1其中R'1和R”1 <1的数值为 或者代表被氟取代的烷基，其具有如上定义的OR 5或NR'R“; e）其中R aa代表氢，烷基或羧基保护基，以及新的中间体化合物的CO 2 CO 2。 式（I）的喹啉是可用于制备具有抗菌活性的化合物的中间体，特别在申请WO 02/40474或WO 02/72572中有所描述。