专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06815548B2 Process for preparing a piperidine derivative 失效
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06815548B2
公开(公告)日：2004-11-09
申请号：US10336678
申请日：2003-01-06
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D40512
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： 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.

2. 发明授权

US06610851B1 Process for preparing a piperidine derivative 失效
标题翻译：哌啶衍生物的制备方法
公开(公告)号：US06610851B1
公开(公告)日：2003-08-26
申请号：US09695383
申请日：2000-10-25
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D40512
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： 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.
摘要翻译：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

US06476227B1 Piperidine derivative and process for preparing the same 失效
标题翻译：哌啶衍生物及其制备方法
公开(公告)号：US06476227B1
公开(公告)日：2002-11-05
申请号：US09550175
申请日：2000-04-14
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D21140
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： 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.
摘要翻译：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。

4. 发明授权

US5948914A Piperidine derivative and process for preparing the same 失效
标题翻译：哌啶衍生物及其制备方法
公开(公告)号：US5948914A
公开(公告)日：1999-09-07
申请号：US53653
申请日：1998-04-02
申请人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
发明人： Kiyoshi Sugi , Nobushige Itaya , Tadashi Katsura , Masami Igi , Shigeya Yamazaki , Taro Ishibashi , Teiji Yamaoka , Yoshihiro Kawada , Yayoi Tagami
IPC分类号： C07D211/22 , C07D211/60 , C07D211/76 , C07D405/12
CPC分类号： C07D405/12 , C07D211/22 , C07D211/60 , C07D211/76
摘要： A piperidine derivative, which can be used as an intermediate for pharmaceuticals such as paroxetine useful as antidepressants, represented by the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, benzyloxycarbonyl group or tert-butoxycarbonyl group; R.sup.2 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 --CO.sub.2 R.sup.7 group in which R.sup.7 is an alkyl group having 1 to 5 carbon atoms, and Z is methylene group or carbonyl group.
摘要翻译：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 R 7为碳原子数为1〜5的烷基，Z为亚甲基或羰基。

5. 发明授权

US06316628B1 L-tartrate of trans-(-)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound and process for preparing the same 失效
标题翻译：反式 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐及其制备方法
公开(公告)号：US06316628B1
公开(公告)日：2001-11-13
申请号：US09342149
申请日：1999-06-29
申请人： Shigeya Yamazaki , Taro Ishibashi , Yoshihiro Kawada , Hiroyuki Yumoto , Taichi Yoshikawa , Masami Igi
发明人： Shigeya Yamazaki , Taro Ishibashi , Yoshihiro Kawada , Hiroyuki Yumoto , Taichi Yoshikawa , Masami Igi
IPC分类号： C07D21122
CPC分类号： C07D211/22
摘要： An L-tartrate of a trans-(−)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound, represented by the formula (I): wherein R1 is hydrogen atom, a substituted or unsubstituted, linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group having 7 to 12 carbon atoms. The L-tartrate of trans-(−)-4-(4-fluorophenyl)-3-hydroxymethylpiperidine compound can be suitably used as an intermediate for pharmaceuticals such as paroxetine which is useful, for example, as an antidepressant.
摘要翻译：由式（I）表示的反 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐：其中R1是氢原子，取代或未取代的直链或支链烷基，其具有 1至6个碳原子，或具有7至12个碳原子的芳烷基。反式 - （ - ） - 4-（4-氟苯基）-3-羟甲基哌啶化合物的L-酒石酸盐可以适当地用作药物例如帕罗西汀的中间体，其可用作例如抗抑郁药。

6. 发明授权

US06433168B1 Highly pure phenothiazine compound, production method thereof, production method of intermediate therefor, and hydrate and novel crystal as starting materials for the intermediate 失效
标题翻译：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
公开(公告)号：US06433168B1
公开(公告)日：2002-08-13
申请号：US09621782
申请日：2000-07-21
申请人： Shigeya Yamazaki , Hiroyuki Yumoto , Masami Igi
发明人： Shigeya Yamazaki , Hiroyuki Yumoto , Masami Igi
IPC分类号： C07D41700
CPC分类号： C07D453/02
摘要： 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.
摘要翻译：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。

7. 发明授权

US06946564B2 Production method of an intermediate for citalopram 失效
标题翻译：西酞普兰中间体的生产方法
公开(公告)号：US06946564B2
公开(公告)日：2005-09-20
申请号：US10744734
申请日：2003-12-23
申请人： Tetsuya Ikemoto , Masami Igi
发明人： Tetsuya Ikemoto , Masami Igi
IPC分类号： C07C29/40 , C07C33/46 , C07C51/265 , C07C51/373 , C07C65/00 , C07C65/34 , C07D307/87 , C07D307/78
CPC分类号： C07D307/87 , C07C29/40 , C07C33/46 , C07C51/265 , C07C51/373 , C07C65/34
摘要： Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.
摘要翻译：通过在N，N，N'，N'-四甲基乙二胺中的至少一种的存在下使下式[Ⅵ]化合物与3-（二甲基氨基）丙基氯反应，可以工业和经济地制备，并以高收率和1,3-二甲基-2-咪唑啉酮和缩合剂。通过使下式[Ⅱ]的化合物还原和环化，可以容易地制备作为西酞普兰生产的关键化合物的下式[III]的化合物。

8. 发明授权

US5440037A Method for production of 2-amino-6-halogenopurine derivatives 失效
标题翻译： 2-氨基-6-卤代嘌呤衍生物的制备方法
公开(公告)号：US5440037A
公开(公告)日：1995-08-08
申请号：US329272
申请日：1994-10-26
申请人： Masami Igi , Taketo Hayashi
发明人： Masami Igi , Taketo Hayashi
IPC分类号： C07D473/40 , C07D473/32
CPC分类号： C07D473/40
摘要： The present invention is directed to a method for production of a 2-amino-6-halogenopurine, a novel synthesis intermediate therefor and a method for production of said synthesis intermediate. The desired 2-amino-6-halogenopurine is an intermediate for the production of the compounds useful as antiviral agents, and by using the compound of the present invention as a starting material, the 2-amino-6-halogenopurine can be produced in high yield.
摘要翻译：本发明涉及2-氨基-6-卤代嘌呤的制备方法，其新型合成中间体及其制备方法。所需的2-氨基-6-卤代嘌呤是用作生产用作抗病毒剂的化合物的中间体，通过使用本发明化合物作为起始原料，2-氨基-6-卤代嘌呤可以以高产量。

9. 发明授权

US5391733A Synthesis intermediates for 2-amino-6-halogenopurines 失效
标题翻译： 2-氨基-6-卤代嘌呤的合成中间体
公开(公告)号：US5391733A
公开(公告)日：1995-02-21
申请号：US937427
申请日：1992-08-31
申请人： Masami Igi , Taketo Hayashi
发明人： Masami Igi , Taketo Hayashi
IPC分类号： C07D473/40 , C07D473/32
CPC分类号： C07D473/40
摘要： The present invention is directed to a method for production of a 2-amino-6-halogenopurine, a novel synthesis intermediate therefor and a method for production of said synthesis intermediate. The desired 2-amino-6-halogenopurine is an intermediate for the production of compounds useful as an antiviral agent, and by using the compound of the present invention as a starting material, the 2-amino-6-halogenopurine can be produced in high yield.
摘要翻译：本发明涉及2-氨基-6-卤代嘌呤的制备方法，其新型合成中间体及其制备方法。所需的2-氨基-6-卤代嘌呤是制备用作抗病毒剂的化合物的中间体，通过使用本发明化合物作为原料，2-氨基-6-卤代嘌呤可以高产产量。

10. 发明授权

US5389637A 2-formylamino-6-halogenopurine 失效
标题翻译： 2-甲酰氨基-6-卤代嘌呤
公开(公告)号：US5389637A
公开(公告)日：1995-02-14
申请号：US115015
申请日：1993-09-02
申请人： Masami Igi , Taketo Hayashi
发明人： Masami Igi , Taketo Hayashi
IPC分类号： C07D473/40
CPC分类号： C07D473/40
摘要： The present invention is directed to a method for production of a 2-amino-6-halogenopurine, a novel synthesis intermediate therefor and a method for production of said synthesis intermediate. The desired 2-amino-6-halogenopurine is an intermediate for the production of compounds useful as antiviral agents, and by using the compound of the present invention as a starting material, the 2-amino-6-halogenopurine can be produced in high yield.
摘要翻译：本发明涉及2-氨基-6-卤代嘌呤的制备方法，其新型合成中间体及其制备方法。所需的2-氨基-6-卤代嘌呤是用于生产可用作抗病毒剂的化合物的中间体，通过使用本发明化合物作为起始原料，可以高产率制备2-氨基-6-卤代嘌呤。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式