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1. 发明授权

US09040745B2 Process for producing fluorosulfuric acid aromatic-ring esters 有权
标题翻译：制备氟代硫酸芳环酯的方法
公开(公告)号：US09040745B2
公开(公告)日：2015-05-26
申请号：US14128362
申请日：2012-06-15
申请人： Akihiro Ishii , Takehisa Ishimaru , Takako Yamazaki , Manabu Yasumoto
发明人： Akihiro Ishii , Takehisa Ishimaru , Takako Yamazaki , Manabu Yasumoto
IPC分类号： C07C303/24
CPC分类号： C07C303/24 , C07C305/26
摘要： A production process of a fluorosulfuric acid aromatic-ring ester according to the present invention includes reaction of an aromatic-ring hydroxyl compound with sulfuryl fluoride (SO2F2) in the presence of a tertiary amine except pyridine and methylpyridine. The sulfuryl fluoride, used as the reactant in the production process according to the present invention, is widely adapted as a fumigant and is easily available on a large scale. Further, the target compound can be obtained rapidly with a high yield under moderate reaction conditions in the production process according to the present invention. In this way, all of the prior art problems can be solved in the production process according to the present invention. The production process according to the present invention is thus particularly useful for industrial production of the fluorosulfuric acid aromatic-ring ester.
摘要翻译：根据本发明的氟代硫酸芳环酯的制备方法包括在除吡啶和甲基吡啶之外的叔胺存在下，芳环羟基化合物与硫酰氟（SO 2 F 2）的反应。在根据本发明的生产方法中用作反应物的硫酰氟被广泛地用作熏蒸剂，并且容易获得大量。此外，在本发明的制造方法中，在中等反应条件下，可以快速获得目标化合物。以这种方式，可以在根据本发明的制造方法中解决所有现有技术问题。因此，本发明的制造方法特别适用于氟代硫酸芳香环酯的工业化生产。

2. 发明申请

US20140114088A1 Process for Producing Fluorosulfuric Acid Aromatic-Ring Esters 有权
标题翻译：生产氟磺酸芳香环酯的方法
公开(公告)号：US20140114088A1
公开(公告)日：2014-04-24
申请号：US14128362
申请日：2012-06-15
申请人： Akihiro Ishii , Takehisa Ishimaru , Takako Yamazaki , Manabu Yasumoto
发明人： Akihiro Ishii , Takehisa Ishimaru , Takako Yamazaki , Manabu Yasumoto
IPC分类号： C07C303/24
CPC分类号： C07C303/24 , C07C305/26
摘要： A production process of a fluorosulfuric acid aromatic-ring ester according to the present invention includes reaction of an aromatic-ring hydroxyl compound with sulfuryl fluoride (SO2F2) in the presence of a tertiary amine except pyridine and methylpyridine. The sulfuryl fluoride, used as the reactant in the production process according to the present invention, is widely adapted as a fumigant and is easily available on a large scale. Further, the target compound can be obtained rapidly with a high yield under moderate reaction conditions in the production process according to the present invention. In this way, all of the prior art problems can be solved in the production process according to the present invention. The production process according to the present invention is thus particularly useful for industrial production of the fluorosulfuric acid aromatic-ring ester.
摘要翻译：根据本发明的氟代硫酸芳环酯的制备方法包括在除吡啶和甲基吡啶之外的叔胺存在下，芳环羟基化合物与硫酰氟（SO 2 F 2）的反应。在根据本发明的生产方法中用作反应物的硫酰氟被广泛地用作熏蒸剂，并且容易获得大量。此外，在本发明的制造方法中，在中等反应条件下，可以快速获得目标化合物。以这种方式，可以在根据本发明的制造方法中解决所有现有技术问题。因此，本发明的制造方法特别适用于氟代硫酸芳香环酯的工业化生产。

3. 发明申请

US20110152536A1 Process for Production of Alpha-Trifluoromethyl-Beta-Substituted-Beta-Amino Acid 有权
标题翻译： α-三氟甲基-β-取代的β-氨基酸的制备方法
公开(公告)号：US20110152536A1
公开(公告)日：2011-06-23
申请号：US13002595
申请日：2009-08-27
申请人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Takashi Masuda
发明人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Takashi Masuda
IPC分类号： C07C229/08 , C07D261/02
CPC分类号： C07D261/04 , C07B53/00 , C07C229/20
摘要： α-Trifluoromethyl-β-substituted-β-amino acids can be produced by allowing α-trifluoromethyl-β-substituted-α,β-unsaturated esters to react with hydroxylamine to convert α-trifluoromethyl-β-substituted-α,β-unsaturated esters into dehydrogenated closed-ring body of α-trifluoromethyl-β-substituted-β-amino acid, and by hydrogenolyzing the dehydrogenated closed-ring body. According to this production process, novel α-trifluoromethyl-β-substituted-β-amino acids which are free amino acids whose functional groups are not protected can be produced, in which β-position substituent is not limited to aromatic ring group or substituted aromatic ring group while the relative stereochemistry of α-position and β-position can be also controlled.
摘要翻译： α-三氟甲基 - 和取代的 - 氨基酸可以通过使α-三氟甲基 - 取代的α，β-不饱和酯与羟胺反应以转化α-三氟甲基 - α，β-不饱和酯转化为α-三氟甲基 - 取代的 - 氨基酸的脱氢闭环体，并通过氢化脱氢闭环体。根据该制造方法，可以制备作为官能团未被保护的游离氨基酸的新型α-三氟甲基 - 取代 - 取代的 - 氨基酸，其中，取代基不限于芳环基或取代的芳族环基团，同时也可以控制相对的立体化学位置和位置。

4. 发明授权

US08653295B2 Process for producing α-trifluoromethyl-α,β-unsaturated ester 有权
标题翻译： α-三氟甲基-α，β-不饱和酯的制备方法
公开(公告)号：US08653295B2
公开(公告)日：2014-02-18
申请号：US13060565
申请日：2009-09-24
申请人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Kazunori Mori , Takashi Masuda
发明人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Kazunori Mori , Takashi Masuda
IPC分类号： C07C69/76
CPC分类号： C07C67/317 , C07C67/327 , C07C69/65
摘要： An α-trifluoromethyl-α,β-unsaturated ester can be produced by reacting an α-trifluoromethyl-α-hydroxy ester with sulfuryl fluoride (SO2F2) in the presence of an organic base. It is preferable that the raw substrate has a hydrogen atom as one β-position substituent group and either an alkyl group, a substituted alkyl group, an alkenyl group, a substituted alkenyl group, an aromatic ring group or a substituted aromatic ring group as the other β-position substituent group. It is more preferable that an ester moiety of the raw substrate is an alkyl ester. This raw substrate is readily available. Further, the desired reaction can proceed favorably with the use of this raw substrate. It is also preferable to use either 1,5-diazabicyclo[4.3.0]non-5-ene (DBN) or 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) as the organic base. The desired reaction can proceed more favorably with the use of this organic base.
摘要翻译： α-三氟甲基-α，β-不饱和酯可以通过在有机碱存在下使α-三氟甲基-α-羟基酯与硫酰氟（SO 2 F 2）反应来制备。原料优选为具有作为一个β位取代基的氢原子，烷基，取代烷基，链烯基，取代烯基，芳香环基或取代芳环基作为其他β位取代基。原料的酯部更优选为烷基酯。该原料基材容易获得。此外，期望的反应可以有利地利用该原始基底进行。还优选使用1,5-二氮杂双环[4.3.0]壬-5-烯（DBN）或1,8-二氮杂双环[5.4.0]十一碳-7-烯（DBU）作为有机碱。使用该有机碱可以更有利地进行所需的反应。

5. 发明授权

US08524913B2 Process for production of α-trifluoromethyl-β-substituted-β-amino acid 有权
标题翻译： α-三氟甲基-β-取代的β-氨基酸的制备方法
公开(公告)号：US08524913B2
公开(公告)日：2013-09-03
申请号：US13002595
申请日：2009-08-27
申请人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Takashi Masuda
发明人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Takashi Masuda
IPC分类号： C07D261/04 , C07C229/20
CPC分类号： C07D261/04 , C07B53/00 , C07C229/20
摘要： α-Trifluoromethyl-β-substituted-β-amino acids can be produced by allowing α-trifluoromethyl-β-substituted-α,β-unsaturated esters to react with hydroxylamine to convert α-trifluoromethyl-β-substituted-α,β-unsaturated esters into dehydrogenated closed-ring body of α-trifluoromethyl-β-substituted-β-amino acid, and by hydrogenolyzing the dehydrogenated closed-ring body. According to this production process, novel α-trifluoromethyl-β-substituted-β-amino acids which are free amino acids whose functional groups are not protected can be produced, in which β-position substituent is not limited to aromatic ring group or substituted aromatic ring group while the relative stereochemistry of α-position and β-position can be also controlled.
摘要翻译： α-三氟甲基-β-取代的β-取代的β-氨基酸可以通过使α-三氟甲基-β-取代的α，β-不饱和酯与羟胺反应以转化α-三氟甲基-β-取代的α，β-不饱和的酯转化成α-三氟甲基-β-取代的β-氨基酸的脱氢闭环体，并通过氢化脱氢闭环体。根据该制造方法，可以制备作为官能团未被保护的游离氨基酸的新型α-三氟甲基-β-取代的β-氨基酸，其中β位取代基不限于芳环或取代芳族环组，而α位和β位的相对立体化学也可以被控制。

6. 发明授权

US08217196B2 Process for producing α-fluoro-β-amino acids 有权
标题翻译：制备α-氟代 - 氨基酸的方法
公开(公告)号：US08217196B2
公开(公告)日：2012-07-10
申请号：US12919108
申请日：2009-04-21
申请人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto , Takashi Masuda , Hideyuki Tsuruta
发明人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto , Takashi Masuda , Hideyuki Tsuruta
IPC分类号： C07C227/16
CPC分类号： C07C227/16 , C07B55/00 , C07C227/32 , C07C229/20
摘要： By reacting a β-hydroxy-α-amino acid with sulfuryl fluoride (SO2F2) in the presence of an organic base, it is possible to produce an α-fluoro-β-amino acid of the formula [2]. By using a C8-12 tertiary amine having two or more alkyl groups of C3 or higher, and especially diisopropylethylamine, as the organic base, by-production of quantery ammonium salts is effectively suppressed. By applying the production process of the present invention, it is possible to very easily produce (2R)-3-(dibenzylamino)-2-fluoropropionic acid methyl ester, which is extremely important as a pharmaceutical intermediate, with high positional selectivity even on an industrial scale.
摘要翻译：通过在有机碱的存在下使β-羟基-α-氨基酸与硫酰氟（SO2F2）反应，可以制备式[2]的α-氟 - 二 - 氨基酸。通过使用具有两个以上具有3个以上的烷基的C8-12叔胺，特别是二异丙基乙胺作为有机碱，有效地抑制了副铵盐的副产物。通过应用本发明的制备方法，可以非常容易地制备作为药物中间体极其重要的（2R）-3-（二苄基氨基）-2-氟丙酸甲酯，即使在工业规模。

7. 发明申请

US20110015428A1 Process for Producing Alpha-Fluoro-Beta-Amino Acids 有权
标题翻译：生产α-氟-β-氨基酸的方法
公开(公告)号：US20110015428A1
公开(公告)日：2011-01-20
申请号：US12919108
申请日：2009-04-21
申请人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto , Takashi Masuda , Hideyuki Tsuruta
发明人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto , Takashi Masuda , Hideyuki Tsuruta
IPC分类号： C07C227/16
CPC分类号： C07C227/16 , C07B55/00 , C07C227/32 , C07C229/20
摘要： By reacting a β-hydroxy-α-amino acid with sulfuryl fluoride (SO2F2) in the presence of an organic base, it is possible to produce an α-fluoro-β-amino acid of the formula [2]. By using a C8-12 tertiary amine having two or more alkyl groups of C3 or higher, and especially diisopropylethylamine, as the organic base, by-production of quantery ammonium salts is effectively suppressed. By applying the production process of the present invention, it is possible to very easily produce (2R)-3-(dibenzylamino)-2-fluoropropionic acid methyl ester, which is extremely important as a pharmaceutical intermediate, with high positional selectivity even on an industrial scale.
摘要翻译：通过在有机碱的存在下使β-羟基-α-氨基酸与硫酰氟（SO2F2）反应，可以制备式[2]的α-氟 - 二 - 氨基酸。通过使用具有两个以上具有3个以上的烷基的C8-12叔胺，特别是二异丙基乙胺作为有机碱，有效地抑制了副铵盐的副产物。通过应用本发明的制备方法，可以非常容易地制备作为药物中间体极其重要的（2R）-3-（二苄基氨基）-2-氟丙酸甲酯，即使在工业规模。

8. 发明授权

US08426645B2 Process for production of optically active fluoroamine 有权
标题翻译：光学活性氟胺的制备方法
公开(公告)号：US08426645B2
公开(公告)日：2013-04-23
申请号：US12919162
申请日：2009-01-27
申请人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto
发明人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto
IPC分类号： C07C257/12 , C07D263/04
CPC分类号： C07B53/00 , C07B2200/07 , C07C209/62 , C07C211/15 , C07C249/02 , C07C251/24
摘要： Disclosed is a process for producing a protected optically active fluoroamine, which comprises the step of reacting an imine-protected optically active hydroxyamine, an oxazolidine-protected optically active hydroxyamine, or a mixture of the imine-protected optically active hydroxyamine and the oxazolidine-protected optically active hydroxyamine, with sulfuryl fluoride (SO2F2) in the presence of a tertiary amine having a carbon number of 7 to 18 (produced by substituting all of three hydrogen atoms in ammonia by alkyl groups). The desired optically active fluoroamine can be produced by hydrolyzing the protected optically active fluoroamine under acidic conditions.
摘要翻译：公开了一种制备受保护的光学活性氟胺的方法，其包括使亚胺保护的光学活性羟胺，恶唑烷保护的光学活性羟胺或亚胺保护的光学活性羟胺与恶唑烷保护的混合物光学活性羟胺与硫酰氟（SO 2 F 2）在碳数为7〜18的叔胺（通过用氨基取代氨基中的全部三个氢原子代替烷基取代）的存在下反应。所需的光学活性氟胺可以通过在酸性条件下水解保护的光学活性氟胺来制备。

9. 发明申请

US20110160477A1 Process for Producing alpha-Trifluoromethyl-alpha,beta-Unsaturated Ester 有权
标题翻译：生产α-三氟甲基-α，β-不饱和酯的方法
公开(公告)号：US20110160477A1
公开(公告)日：2011-06-30
申请号：US13060565
申请日：2009-09-24
申请人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Kazunori Mori , Takashi Masuda
发明人： Akihiro Ishii , Manabu Yasumoto , Takako Yamazaki , Kaori Mogi , Kazunori Mori , Takashi Masuda
IPC分类号： C07C67/327
CPC分类号： C07C67/317 , C07C67/327 , C07C69/65
摘要： An α-trifluoromethyl-α,β-unsaturated ester can be produced by reacting an α-trifluoromethyl-α-hydroxy ester with sulfuryl fluoride (SO2F2) in the presence of an organic base. It is preferable that the raw substrate has a hydrogen atom as one β-position substituent group and either an alkyl group, a substituted alkyl group, an alkenyl group, a substituted alkenyl group, an aromatic ring group or a substituted aromatic ring group as the other β-position substituent group. It is more preferable that an ester moiety of the raw substrate is an alkyl ester. This raw substrate is readily available. Further, the desired reaction can proceed favorably with the use of this raw substrate. It is also preferable to use either 1,5-diazabicyclo[4.3.0]non-5-ene (DBN) or 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) as the organic base. The desired reaction can proceed more favorably with the use of this organic base.
摘要翻译： α-三氟甲基-α，β-不饱和酯可以通过α-三氟甲基-α-羟基酯与硫酰氟（SO 2 F 2）在有机碱的存在下反应来制备。原料优选为氢原子作为一个位置取代基和烷基，取代的烷基，链烯基，取代的烯基，芳族环基或取代的芳环基作为另一个位置取代基。原料的酯部更优选为烷基酯。该原料基材容易获得。此外，期望的反应可以有利地利用该原始基底进行。还优选使用1,5-二氮杂双环[4.3.0]壬-5-烯（DBN）或1,8-二氮杂双环[5.4.0]十一碳-7-烯（DBU）作为有机碱。使用该有机碱可以更有利地进行所需的反应。

10. 发明申请

US20110034732A1 Process for Production of Optically Active Fluoroamine 有权
标题翻译：光活性氟胺的生产工艺
公开(公告)号：US20110034732A1
公开(公告)日：2011-02-10
申请号：US12919162
申请日：2009-01-27
申请人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto
发明人： Akihiro Ishii , Takako Yamazaki , Manabu Yasumoto
IPC分类号： C07C251/16 , C07C249/02 , C07C209/68
CPC分类号： C07B53/00 , C07B2200/07 , C07C209/62 , C07C211/15 , C07C249/02 , C07C251/24
摘要： Disclosed is a process for producing a protected optically active fluoroamine, which comprises the step of reacting an imine-protected optically active hydroxyamine, an oxazolidine-protected optically active hydroxyamine, or a mixture of the imine-protected optically active hydroxyamine and the oxazolidine-protected optically active hydroxyamine, with sulfuryl fluoride (SO2F2) in the presence of a tertiary amine having a carbon number of 7 to 18 (produced by substituting all of three hydrogen atoms in ammonia by alkyl groups). The desired optically active fluoroamine can be produced by hydrolyzing the protected optically active fluoroamine under acidic conditions.
摘要翻译：公开了一种制备受保护的光学活性氟胺的方法，其包括使亚胺保护的光学活性羟胺，恶唑烷保护的光学活性羟胺或亚胺保护的光学活性羟胺与恶唑烷保护的混合物光学活性羟胺与硫酰氟（SO 2 F 2）在碳数为7〜18的叔胺（通过用氨基取代氨基中的全部三个氢原子代替烷基取代）的存在下反应。所需的光学活性氟胺可以通过在酸性条件下水解保护的光学活性氟胺来制备。

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