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    NEW HYDROXYPHENYL DERIVATIVES AND BIOLOGICAL APPLICATIONS THEREOF
    2.
    发明申请
    NEW HYDROXYPHENYL DERIVATIVES AND BIOLOGICAL APPLICATIONS THEREOF 审中-公开
    新型羟基衍生物及其生物应用

    公开(公告)号：WO2007135562A2

    公开(公告)日：2007-11-29

    申请号：PCT/IB2007002127

    申请日：2007-04-16

    申请人： MUTABILIS S A ,  DENIS ALEXIS ,  GERUSZ VINCENT ,  BONVIN YANNICK

    发明人： DENIS ALEXIS ,  GERUSZ VINCENT ,  BONVIN YANNICK

    IPC分类号： C07D213/643 ,  C07C43/263 ,  C07C49/84 ,  C07C69/24 ,  C07C211/52 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75

    CPC分类号： C07D213/643 ,  C07C41/16 ,  C07C41/26 ,  C07C43/23 ,  C07C43/275 ,  C07C43/295 ,  C07C45/673 ,  C07C45/71 ,  C07C49/84 ,  C07C205/38 ,  C07C209/08 ,  C07C209/14 ,  C07C217/90 ,  C07C251/54 ,  C07C309/73 ,  C07D209/50 ,  C07D213/68 ,  C07D213/69 ,  C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/76 ,  C07D295/092 ,  C07D295/16 ,  C07D401/12

    摘要： The invention relates to hydroxyphenyl derivatives of formula (I) wherein R1 is phenyl or a 6 membered monocyclic nitrogenous heteroaryl of formula wherein Z4, Z5, Z6, Z7 and Z8 are C or N with a maximum of three N, R1 being possibly substituted by 1 to 3 R identical or different, - R2 is phenyl, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, C 1 - C 4 f luoro-alkyl, C 2 -C 4 f luoro-alkenyl, OR 3 , SR a , all being possibly substituted by 1 to 3 identical or different R', - R a ,R b and R c , are H, C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, phenyl, heteroaryl and aliphatic heterocycle as defined above for R2, the heteroaryl and the heterocycle being possibly formed with the carbon and nitrogen atoms to which R a , R b and R c are linked, - R' is heteroaryl and aliphatic heterocycle as defined above for R2, C 1 -C 8 alkyl, CH 2 CO 2 R", CO 2 R", COR", CONR"R"', OCOR", OR", NR"R"', NR"C0R'", NR"COOR"', OCONR"R"', NR"CONR"R"', NR"SO 2 R"', SO 2 R", NR"SO 2 R"', halogen and CN, R" and R"', identical or different, are H, C 1 -C 8 alkyl or form together a 4 to 6 membered heterocycle with 1 to 3 heteroatoms selected from N, 0 and S, - Y represents H or a labile chemical group able to regenerate in vivo the free phenol - Z1 and Z3 are halogen or H, and Z2 is fluor or H, provided that - either Z2 is fluor and all the other definitions are as defined above, - or Z6 is a carbon atom substituted by R as defined above, R being different from H, alkyl, halogen, NH2, OH, CONH 2 or fluoro alkyl and all the other definitions are as defined above, - or Z4 or Z5, or Z7 or Z8 are carbon atoms substituted by NR a R b or OR a , OR a being different from OH and all the other definitions are as defined above, - or Z5, or Z7, is a carbon atom substituted by R, R being different from H and all the other definitions are as defined above, - or R2 is a C 1 -C 8 alkyl-heteroaryl radical or a C 1 - C 8 alkyl-OR a radical, 0R a being different from OH and all the other definitions are as defined above. Applications as anti-bacterial and/or anti-parasites agents.

    摘要翻译： 本发明涉及式（I）的羟基苯基衍生物，其中R 1是苯基或下式的6元单环含氮杂芳基其中Z4，Z5，Z6，Z7和Z8是C或N，最多三个N，R 1可以被 1至3个R相同或不同，-R 2是苯基，C 1 -C 8烷基，C 2 -C 8烷基， 亚烷基，C 2 -C 8炔基，C 1 -C 4烷基，C 1 -C 4烷基， C 2 -C 4 - 烯基，OR 3，SR a，全部可被1个 至3个相同或不同的R 1，R 2，R b和R c是H，C 1 H C 1 -C 8烷基，C 2 -C 8链烯基，C 2 -C 8烷基，C 2 -C 8烷基， R 1，R 2，R 3，R 3，R 3，R 3，R 3，R 3，R 3，R 3， SUB和R c连接，-R'是H. 芳基和脂族杂环如上面对于R 2，C 1 -C 8烷基，CH 2 CO 2 R 2， “，CO 2”R“，COR”，CONR“R”'，OCOR“，OR”，NR“R”'，NR“C0R”，NR“COOR”，OCONR“R “'，NR”CONR“R”'，NR“SO 2 R”'，SO 2 R“，NR”SO 2 R “'，卤素和CN，R”和R“'相同或不同，为H，C 1 -C 8烷基或一起形成4至6元杂环 具有1至3个选自N，O和S的杂原子，Y表示H或能够在体内再生的不稳定化学基团，游离苯酚-Z 1和Z 3为卤素或H，Z 2为氟或H，条件是 - Z2是氟并且所有其它定义如上所定义， - 或Z6是被如上定义的R取代的碳原子，R不同于H，烷基，卤素，NH 2，OH，CONH 2 或氟烷基，所有其它定义如上所定义， - 或Z 4或Z 5或Z 7或Z 8为被NR a R b取代的碳原子或OR >一或OR a不同于OH，所有其它定义如上所定义， - 或Z5或Z7为被R取代的碳原子，R不同于H，所有其它 定义如上所定义， - 或R 2是C 1 -C 8烷基 - 杂芳基或C 1 -C 6 - 8烷基-OR aα，O R a不同于OH，并且所有其它定义如上所定义。 用作抗菌和/或抗寄生虫剂。

    PROCESS FOR PRODUCING 4-SUBSTITUTED-2-NITRO-FLUOROBENZENES
    4.
    发明申请
    PROCESS FOR PRODUCING 4-SUBSTITUTED-2-NITRO-FLUOROBENZENES 审中-公开
    生产4-取代-2-硝基苯并噻唑的方法

    公开(公告)号：WO00003971A1

    公开(公告)日：2000-01-27

    申请号：PCT/JP1999/003825

    申请日：1999-07-15

    IPC分类号： C07C201/08 ,  C07C201/16 ,  C07C205/12 ,  C07C205/37 ,  C07C205/38 ,  C07C205/43 ,  C07C205/45 ,  C07C205/58 ,  C07D401/10 ,  A61K31/44 ,  C07D205/12

    CPC分类号： C07D401/10 ,  C07C201/08 ,  C07C201/12 ,  C07C201/16 ,  C07C205/58 ,  C07C205/43 ,  C07C205/38 ,  C07C205/37 ,  C07C205/45 ,  C07C205/12

    摘要： A process for selectively eliminating a compound of general formula (II) from a mixture of a compound of general formula (I) with the compound of general formula (II). This process comprises reacting the compound of general formula (II) with a tertiary amine and a nucleophilic agent and then washing and/or crystallizing the thus obtained compound to thereby separate the same from the mixture. A process for producing a compound represented by general formula (I) which is free from any mutagen is also provided. In these formulae, R represents alkyl, alkyl carbonyl or alkoxycarbonyl; and Hal represents halogeno.

    摘要翻译： 从通式（I）的化合物与通式（II）的化合物的混合物中选择性地除去通式（II）的化合物的方法。 该方法包括使通式（II）的化合物与叔胺和亲核试剂反应，然后将由此得到的化合物洗涤和/或结晶，从而将其与混合物分离。 还提供了不含任何诱变剂的由通式（I）表示的化合物的制备方法。 在这些式中，R 1表示烷基，烷基羰基或烷氧基羰基; 而Hal代表卤代。