Trifluorovinyloxy-n-monoalkylaniline compound and method for producing the same
    4.
    发明专利
    Trifluorovinyloxy-n-monoalkylaniline compound and method for producing the same 有权
    三氟乙烯基-N-单甲基兰兰化合物及其制备方法

    公开(公告)号:JP2011213642A

    公开(公告)日:2011-10-27

    申请号:JP2010082493

    申请日:2010-03-31

    发明人: SAITO SATOSHI

    摘要: PROBLEM TO BE SOLVED: To provide a trifluorovinyloxyaniline compound which achieves the reduction of the viscosity of a fluorine-containing polyether compound into which a trifluorovinyloxyaniline compound has been introduced as reaction sites at both terminals of the polymer main chain and a method for producing the same.SOLUTION: The trifluorovinyloxy-N-monoalkylaniline compound is represented by formula [I] (wherein Ris a 1-3C alkyl group) and is preferably trifluorovinyloxy-N-monomethylaniline. This trifluorovinyloxy-N-monoalkylaniline is produced by the method for N-monoalkylating trifluorovinyloxyaniline or the method for N-monoalkylating (2-bromotetrafluoroethoxy)aniline of the precursor of trifluorovinyloxyaniline and thereafter subjecting the resulting (2-bromotetrafluoroethoxy)-N-monoalkylaniline to the FBr elimination reaction.

    摘要翻译: 要解决的问题:提供一种三聚乙烯氧基苯胺化合物,其实现了引入三氟乙烯氧基苯胺化合物的含氟聚醚化合物的粘度降低,作为聚合物主链两端的反应位点及其制备方法 溶液:三氟乙烯基-N-单烷基苯胺化合物由式[I]表示(其中,R 1为1-3C烷基),优选为三氟乙烯基氧基-N-单甲基苯胺。 该三氟乙烯基-N-单烷基苯胺通过三氟乙烯氧基苯胺的N-单烷基化方法或三氟乙烯氧基苯胺前体的N-单烷基化(2-溴四氟乙氧基)苯胺的方法制备,然后将得到的(2-溴四氟乙氧基)-N-单烷基苯胺 FBr消除反应。

    A process for the preparation of combretastatin

    公开(公告)号:JP2011513286A

    公开(公告)日:2011-04-28

    申请号:JP2010548144

    申请日:2009-02-27

    摘要: Enrichment of a salt of amino compound (I) in isomer (Z), comprises adding benzyl alcohol to a suspension of a mixture of salts of (Z)- and (E)- amino compounds in acetonitrile, and mechanically separating the salt of the amino compound enriched in isomer (Z). Enrichment of salt of amino compound of formula (I) in isomer (Z), comprises adding benzyl alcohol to a suspension of a mixture of salts of (Z)- and (E)- amino compounds in acetonitrile, and mechanically separating the salt of the amino compound enriched in isomer (Z).B 1>= counter-anion, preferably Cl ->or SO 4 2> ->. Independent claims are included for: (1) a process for the preparation of a combretastatin of formula (Z)-(Ic) comprising: coupling the salt of (Z)- amino compound (I) with doubly protected L-serine derivative of formula (II) to obtain the combretastatin compound of formula (Z)-(Ib), then deprotecting and opening the (Z)-(Ib) cycle; or enriching (I), coupling the enriched salt with (II) in the presence of propane phosphonic acid anhydride (T3P) of formula (III) to obtain (Z)-(Ib), and then deprotecting and opening the cycle (Z)-(lb); or coupling salt of (Z)-amino compound of formula (IV) with (II) in the presence of (III) to obtain (Z)-(Ib) and then deprotecting and opening the (Z)-(lb) cycle; and (2) use of (III) for carrying out the coupling of (IV) with the double protected L-serine derivative (II). PG : protective group of the amino function, preferably tert-butoxycarbonyl, benzyloxycarbonyl or 9-fluorenylmethyloxycarbonyl. [Image] [Image] [Image] [Image] [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : None given.

    METHOD FOR PRODUCING 2,5-DIAMINOHYDROQUINONE AND/OR ITS ESTER OR THEIR SALTS

    公开(公告)号:JP2001354633A

    公开(公告)日:2001-12-25

    申请号:JP2000181900

    申请日:2000-06-16

    申请人: TOYO BOSEKI

    摘要: PROBLEM TO BE SOLVED: To simply and inexpensively produce 2 5-diamino-hydroquinone and/or its ether or their salts useful as a monomer for a heat-resistant polymer polybenzoxazole(PBO) and a dye intermediate by one process. SOLUTION: This method for producing 2,5-diamino-hydroquinone of general formula (3) and/or its ether or their salts comprises reducing a 2-alkoxy-4- nitroaniline and/or 2-hydroxy-4-nitroaniline of general formula (1) in which the para-position of OR1 group is nonsubstituted with a reducing agent in a reaction solvent, then, without isolation, to give a reaction intermediate of general formula (2) (R1 and R2 are each hydrogen or a 1-4C alkyl; R3 is a 1-4C alkyl; the para-position of OR1 is nonsubstituted; X and Y are each hydrogen or a 1-4C alkyl; during the reaction process, not necessarily X is R1 and Y is R2; n is an integer of 0, 1 or 2) and carrying out a rearrangement reaction by heat and/or an acid catalyst.