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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明授权

US07119215B2 Production method of citalopram, intermediate therefor and production method of the intermediate 失效
标题翻译：西酞普兰的生产方法，中间体和中间体的生产方法
公开(公告)号：US07119215B2
公开(公告)日：2006-10-10
申请号：US10086076
申请日：2002-02-28
申请人： Tetsuya Ikemoto , Wei-Guo Gao , Masami Igi
发明人： Tetsuya Ikemoto , Wei-Guo Gao , Masami Igi
IPC分类号： C07D307/78
CPC分类号： C07D307/87 , C07C29/40 , C07C33/46 , C07C51/265 , C07C51/373 , C07C65/34
摘要： A compound of formula [V] is prepared by oxidizing a compound of formula [III]. Citalopram can be industrially and economically produced and at a high yield by converting a compound of formula [V], which is prepared from a compound of formula [III], to a compound of formula [VI], and then alkylating the compound of formula [VI] to form citalopram.
摘要翻译：通过氧化式[III]化合物制备式[Ⅴ]化合物。西酞普兰可以通过将由式[Ⅲ]化合物制备的式[Ⅴ]化合物转化成式[Ⅵ]化合物，从而可以在工业和经济上产生并以高收率，然后将式 [六]形成西酞普兰。

6. 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.

7. 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。

8. 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。

9. 发明申请

US20060167285A1 Production methods of citalopram and intermediates therefor 审中-公开
标题翻译：西酞普兰及其中间体的生产方法
公开(公告)号：US20060167285A1
公开(公告)日：2006-07-27
申请号：US11386018
申请日：2006-03-21
申请人： Tetsuya Ikemoto , Masami Igi
发明人： Tetsuya Ikemoto , Masami Igi
IPC分类号： C07D307/87
CPC分类号： C07D307/79 , C07C29/095 , C07C33/46 , C07C43/313 , C07C69/63 , C07C2601/16 , C07D307/87
摘要： The present invention provides a production method of citalopram and intermediates therefor.
摘要翻译：本发明提供西酞普兰及其中间体的制备方法。

10. 发明申请

US20050080278A1 Production methods of citalopram and intermediates therefor 审中-公开
标题翻译：西酞普兰及其中间体的生产方法
公开(公告)号：US20050080278A1
公开(公告)日：2005-04-14
申请号：US10650875
申请日：2003-08-28
申请人： Tetsuya Ikemoto , Masami Igi
发明人： Tetsuya Ikemoto , Masami Igi
IPC分类号： C07C27/02 , C07C29/09 , C07C33/46 , C07C41/06 , C07C41/16 , C07C43/174 , C07C43/303 , C07C43/313 , C07C67/287 , C07C69/63 , C07D307/79 , C07D307/87 , C07C33/26
CPC分类号： C07D307/79 , C07C29/095 , C07C33/46 , C07C43/313 , C07C69/63 , C07C2601/16 , C07D307/87
摘要： The present invention provides a production method of citalopram and intermediates therefor.
摘要翻译：本发明提供西酞普兰及其中间体的制备方法。

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