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    • 2. 发明授权
    • Process for preparing a piperidine derivative
    • 哌啶衍生物的制备方法
    • US06610851B1
    • 2003-08-26
    • US09695383
    • 2000-10-25
    • Kiyoshi SugiNobushige ItayaTadashi KatsuraMasami IgiShigeya YamazakiTaro IshibashiTeiji YamaokaYoshihiro KawadaYayoi Tagami
    • Kiyoshi SugiNobushige ItayaTadashi KatsuraMasami IgiShigeya YamazakiTaro IshibashiTeiji YamaokaYoshihiro KawadaYayoi Tagami
    • C07D40512
    • C07D405/12C07D211/22C07D211/60C07D211/76
    • A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is carbonyl group, then R2 is carboxyl group or —CO2R7 group (R7 is as defined above); or (C) when R1 is hydrogen atom and Z is methylene group, then R2 is hydroxymethyl group.
    • 哌啶衍生物,其可以用作药物的中间体,例如用作抗抑郁药的帕罗西汀,由通式(I)表示:其中R1是氢原子,苄氧基羰基或叔丁氧基羰基; R2是羟甲基,具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基,4-位可具有甲基的苯基磺酰氧基甲基,(3,4-亚甲二氧基苯基)氧甲基,羧基或-CO 2 R 7基,其中 R7为碳原子数为1〜5的烷基,Z为亚甲基或羰基,条件是(A)当R1为苄氧羰基或叔丁氧基羰基时,则R2为羟甲基,烷基磺酰氧基甲基为 具有1至2个碳原子的烷基部分,可以在4-位具有甲基的苯基磺酰氧基甲基或(3,4-亚甲二氧基苯基)氧基甲基,Z是亚甲基; 或(B)当R 1为氢原子且Z为羰基时,则R 2为羧基或-CO 2 R 7基(R 7如上所定义); 或(C)当R 1为氢原子且Z为亚甲基时,则R 2为羟甲基。
    • 3. 发明授权
    • Piperidine derivative and process for preparing the same
    • 哌啶衍生物及其制备方法
    • US06476227B1
    • 2002-11-05
    • US09550175
    • 2000-04-14
    • Kiyoshi SugiNobushige ItayaTadashi KatsuraMasami IgiShigeya YamazakiTaro IshibashiTeiji YamaokaYoshihiro KawadaYayoi Tagami
    • Kiyoshi SugiNobushige ItayaTadashi KatsuraMasami IgiShigeya YamazakiTaro IshibashiTeiji YamaokaYoshihiro KawadaYayoi Tagami
    • C07D21140
    • C07D405/12C07D211/22C07D211/60C07D211/76
    • A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): wherein R1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position, (3,4-methylenedioxyphenyl)oxymethyl group, carboxyl group or —CO2R7 group in which R7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group, with proviso that, (A) when R1 is benzyloxycarbonyl group or tert-butoxycarbonyl group, then R2 is hydroxymethyl group, an alkylsulfonyloxymethyl group having an alkyl moiety of 1 to 2 carbon atoms, phenylsulfonyloxymethyl group which may have methyl group at the 4-position or (3,4-methylenedioxyphenyl)oxymethyl group, and Z is methylene group; or (B) when R1 is hydrogen atom and Z is carbonyl group, then R2 is carboxyl group or —CO2R7 group (R7 is as defined above); or (C) when R1 is hydrogen atom and Z is methylene group, then R2 is hydroxymethyl group.
    • 哌啶衍生物,其可以用作药物的中间体,例如用作抗抑郁药的帕罗西汀,由通式(I)表示:其中R1是氢原子,苄氧基羰基或叔丁氧基羰基; R2是羟甲基,具有1〜2个碳原子的烷基部分的烷基磺酰氧基甲基,4-位可具有甲基的苯基磺酰氧基甲基,(3,4-亚甲二氧基苯基)氧甲基,羧基或-CO 2 R 7基,其中 R7为碳原子数为1〜5的烷基,Z为亚甲基或羰基,条件是(A)当R1为苄氧羰基或叔丁氧基羰基时,则R2为羟甲基,烷基磺酰氧基甲基为 具有1至2个碳原子的烷基部分,可以在4-位具有甲基的苯基磺酰氧基甲基或(3,4-亚甲二氧基苯基)氧基甲基,Z是亚甲基; 或(B)当R 1为氢原子且Z为羰基时,则R 2为羧基或-CO 2 R 7基(R 7如上所定义); 或(C)当R 1为氢原子且Z为亚甲基时,则R 2为羟甲基。
    • 6. 发明授权
    • Highly pure phenothiazine compound, production method thereof, production method of intermediate therefor, and hydrate and novel crystal as starting materials for the intermediate
    • 高纯吩噻嗪化合物,其制备方法,其中间体的制备方法,水合物和新型晶体为中间体的起始原料
    • US06433168B1
    • 2002-08-13
    • US09621782
    • 2000-07-21
    • Shigeya YamazakiHiroyuki YumotoMasami Igi
    • Shigeya YamazakiHiroyuki YumotoMasami Igi
    • C07D41700
    • C07D453/02
    • According to the method of the present invention, an alkali metal compound, dimethyl sulfoxide, trimethyloxosulfonium halide and 3-quinuclidinone are added in a specific order to give the following compound [II]. This compound is, without treatment or isolation, directly reacted with an alkali metal salt of phenothiazine to give the following compound [III], from which the following compound [I] is obtained. During the production of compound [I], a by-produced acidic gas is removed and water is added to ensure industrial, safe and efficient production of compound [I] at a constantly high yield. Inasmuch as the present invention enables production of the following highly pure compound [A] by eliminating hydrogen halide of compound [I] in glyme in the presence of at least one kind of a base selected from potassium hydroxide and potassium alkoxide, compound [A] having a high purity of not less than 85 mol % can be provided.
    • 根据本发明的方法,以特定的顺序加入碱金属化合物,二甲基亚砜,三甲基锍卤化物和3-奎宁环酮,得到下列化合物[II]。 该化合物在不经处理或分离的情况下与吩噻嗪的碱金属盐直接反应,得到以下化合物[III],由此得到下列化合物[I]。 在化合物[I]的生产过程中,除去副产的酸性气体,加入水以确保化合物[I]的工业,安全和有效的生产以不断的高产率。 由于本发明能够通过在至少一种选自氢氧化钾和醇钾的碱的存在下,通过除去甘醇二甲醚中的化合物[I]的卤化氢来制备下列高纯度化合物[A],化合物[A] 可以提供不小于85mol%的高纯度。