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1. 发明申请

US20050148801A1 Optically active nitro alcohol derivatives, optically active amino alcohol derivatives, and process for producing thereof 有权
标题翻译：光学活性硝基醇衍生物，光学活性氨基醇衍生物及其制备方法
公开(公告)号：US20050148801A1
公开(公告)日：2005-07-07
申请号：US11044223
申请日：2005-01-28
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
IPC分类号： C07C201/12 , C07C205/16 , C07C205/17 , C07C205/37 , C07C205/42 , C07C213/02 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07D319/08 , C07F7/18 , C07C25/16
CPC分类号： C07D319/08 , B01J31/223 , B01J2231/342 , B01J2531/0266 , B01J2531/37 , B01J2531/38 , C07B2200/07 , C07C205/16 , C07C205/17 , C07C205/35 , C07C205/37 , C07C205/40 , C07C205/42 , C07C213/02 , C07C215/60 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07F7/1804 , C07F7/1892
摘要： Optically active 1-substituted phenyl-2-nitro alcohol derivatives having the formula (1) and the process for producing thereof, and 1-substituted phenyl-2-amino alcohol derivatives having the formula (2) and the process for producing thereof from the optically active 1-substituted phenyl-2-nitro alcohol derivatives. From these nitro alcohols, pharmaceuticals such as (R)-albutamin and (R)-sarmeterol useful as a bronchodilator is obtained via optically active amino alcohols which are useful pharmaceutical intermediates.
摘要翻译：具有式（1）的光学活性1-取代苯基-2-硝基醇衍生物及其制备方法和具有式（2）的1-取代苯基-2-氨基醇衍生物及其制备方法光学活性的1-取代苯基-2-硝基醇衍生物。通过这些硝基醇，可以通过作为有用的药物中间体的光学活性氨基醇获得用作支气管扩张剂的（R） - 丁二胺和（R） - 三异胺的药物。

2. 发明申请

US20070060656A1 Optically active nitro alcohol derivatives, optically active amino alcohol derivatives, and process for producing thereof 审中-公开
标题翻译：光学活性硝基醇衍生物，光学活性氨基醇衍生物及其制备方法
公开(公告)号：US20070060656A1
公开(公告)日：2007-03-15
申请号：US11595987
申请日：2006-11-13
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
IPC分类号： A61K31/138 , C07C205/16
CPC分类号： C07D319/08 , B01J31/223 , B01J2231/342 , B01J2531/0266 , B01J2531/37 , B01J2531/38 , C07B2200/07 , C07C205/16 , C07C205/17 , C07C205/35 , C07C205/37 , C07C205/40 , C07C205/42 , C07C213/02 , C07C215/60 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07F7/1804 , C07F7/1892
摘要： Optically active 1-substituted phenyl-2-nitro alcohol derivatives having the formula (1) and the process for producing thereof, and 1-substituted phenyl-2-amino alcohol derivatives having the formula (2) and the process for producing thereof from the optically active 1-substituted phenyl-2-nitro alcohol derivatives. From these nitro alcohols, pharmaceuticals such as (R)-albutamin and (R)-sarmeterol useful as a bronchodilator is obtained via optically active amino alcohols which are useful pharmaceutical intermediates.
摘要翻译：具有式（1）的光学活性1-取代苯基-2-硝基醇衍生物及其制备方法和具有式（2）的1-取代苯基-2-氨基醇衍生物及其制备方法光学活性的1-取代苯基-2-硝基醇衍生物。通过这些硝基醇，可以通过作为有用的药物中间体的光学活性氨基醇获得用作支气管扩张剂的（R） - 丁二胺和（R） - 三异胺的药物。

3. 发明授权

US06632955B1 Optically active nitro alcohol derivatives, optically active amino alcohol derivatives, and process for preparing the same 失效
标题翻译：光学活性硝基醇衍生物，光学活性氨基醇衍生物及其制备方法
公开(公告)号：US06632955B1
公开(公告)日：2003-10-14
申请号：US09319135
申请日：1999-09-01
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
IPC分类号： C07F704
CPC分类号： C07D319/08 , B01J31/223 , B01J2231/342 , B01J2531/0266 , B01J2531/37 , B01J2531/38 , C07B2200/07 , C07C205/16 , C07C205/17 , C07C205/35 , C07C205/37 , C07C205/40 , C07C205/42 , C07C213/02 , C07C215/60 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07F7/1804 , C07F7/1892
摘要： Optically active 1-substituted phenyl-2-nitro alcohol derivatives having the formula (1) and the process for producing thereof, and 1-substituted phenyl-2-amino alcohol derivatives having the formula (2) and the process for producing thereof from the optically active 1-substituted phenyl-2-nitro alcohol derivatives. From these nitro alcohols, pharmaceuticals such as (R)-albutamin and (R)-sarmeterol useful as a bronchodilator is obtained via optically active amino alcohols which are useful pharmaceutical intermediates.
摘要翻译：具有式（1）的光学活性1-取代苯基-2-硝基醇衍生物及其制备方法和具有式（2）的1-取代苯基-2-氨基醇衍生物及其制备方法光学活性的1-取代苯基-2-硝基醇衍生物。通过这些硝基醇，可以通过作为有用的药物中间体的光学活性氨基醇获得用作支气管扩张剂的（R） - 丁二胺和（R） - 三异胺的药物。

4. 发明授权

US07205425B2 Optically active nitro alcohol derivatives, optically active amino alcohol derivatives, and process for producing thereof 有权
标题翻译：光学活性硝基醇衍生物，光学活性氨基醇衍生物及其制备方法
公开(公告)号：US07205425B2
公开(公告)日：2007-04-17
申请号：US11044223
申请日：2005-01-28
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Yasuo Urata , Mamoru Fujita
IPC分类号： C07F7/04
CPC分类号： C07D319/08 , B01J31/223 , B01J2231/342 , B01J2531/0266 , B01J2531/37 , B01J2531/38 , C07B2200/07 , C07C205/16 , C07C205/17 , C07C205/35 , C07C205/37 , C07C205/40 , C07C205/42 , C07C213/02 , C07C215/60 , C07C217/10 , C07C217/70 , C07C219/30 , C07D317/54 , C07F7/1804 , C07F7/1892
摘要： Optically active 1-substituted phenyl-2-nitro alcohol derivatives having the formula (1) and the process for producing thereof, and 1-substituted phenyl-2-amino alcohol derivatives having the formula (2) and the process for producing thereof from the optically active 1-substituted phenyl-2-nitro alcohol derivatives. From these nitro alcohols, pharmaceuticals such as (R)-albutamin and (R)-sarmeterol useful as a bronchodilator is obtained via optically active amino alcohols which are useful pharmaceutical intermediates.
摘要翻译：具有式（1）的光学活性1-取代苯基-2-硝基醇衍生物

5. 发明授权

US6090969A Process for the preparation of an asymmetric compound using a metal complex 失效
标题翻译：使用金属络合物制备不对称化合物的方法
公开(公告)号：US6090969A
公开(公告)日：2000-07-18
申请号：US149735
申请日：1998-09-08
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Takayoshi Arai
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Takayoshi Arai
IPC分类号： B01J31/22 , B01J31/02 , B01J31/14 , C07B53/00 , C07B61/00 , C07C67/333 , C07C67/347 , C07C69/716 , C07C69/738 , C07F9/40 , C07C255/00 , C07C39/14 , C07C41/00
CPC分类号： C07F9/4056 , B01J31/143 , B01J31/1805 , B01J31/223 , C07B53/00 , C07C67/347 , C07F9/4006 , C07F9/4015 , C07F9/4018 , B01J2231/323 , B01J2231/341 , B01J2231/348 , B01J2531/0266 , B01J2531/11 , B01J2531/31
摘要： A process for producing an asymmetric compound using a metal complex containing no rare earth metal element is disclosed. The process affords an optically active compound having high optical purity. Optically active binaphthol having the chemical formula and lithium aluminum hydride are reacted, or the optically active binaphthol, a dialkyl aluminum hydride, and a base containing an alkali metal (or a base containing alkaline earth metal) are reacted to prepare a metal complex comprising optically active binaphthol, aluminum, and alkali metal (or alkaline earth metal). This metal complex can be used as a catalyst to perform an asymmetric Michael reaction, an asymmetric phosphonylation reaction, or the like, to obtain, in a high yield, an asymmetric compound having high optical purity.
摘要翻译：公开了使用不含稀土金属元素的金属络合物制造不对称化合物的方法。该方法提供具有高光学纯度的光学活性化合物。使具有化学式和氢化锂铝的光学活性联萘酚反应，或光学活性联萘酚，二烷基氢化铝和含有碱金属（或碱土金属的碱）的碱反应以制备包含光学的金属络合物活性联萘酚，铝和碱金属（或碱土金属）。该金属络合物可用作催化剂进行不对称迈克尔反应，不对称膦酰化反应等，以高产率获得具有高光学纯度的不对称化合物。

6. 发明授权

US6084123A Process for the preparation of optically active 1-aminophosphonic acid derivatives and novel phosphonate compounds 失效
标题翻译：光学活性1-氨基膦酸衍生物和新型膦酸酯化合物的制备方法
公开(公告)号：US6084123A
公开(公告)日：2000-07-04
申请号：US043678
申请日：1998-05-20
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Yoshihiro Tahara
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Yoshihiro Tahara
IPC分类号： C07F9/38 , C07F9/40 , C07F9/44
CPC分类号： C07F9/4006 , C07F9/3808
摘要： Provided is a process for the preparation of an optically active (R)- or (S)-1-aminophosphonic acid derivative of the general formula (Ia) or (Ib) given below, which process comprises reacting an amino-protected imine having general formula (II): R.sup.1 --N.dbd.CHR.sup.2 where R.sup.1 is diphenylmethyl group or the like and R.sup.2 is an alkyl group or the like, with a phosphonic acid ester in the presence of an asymmetric catalyst consisting of a rare earth element-alkali metal-binaphthol complex, to produce an (R)- or (S)-N-protected-1-aminophosphonate compound, and then subjecting the phosphonate compound to catalytic reduction with hydrogen and to acidic hydrolysis. ##STR1## There are also provided novel intermediates, and a process of preparing an asymmetric catalyst consisting of a rare element-alkali metal-binaphthol complex.
摘要翻译： PCT No.PCT / JP96 / 02794 Sec。 371日期：1998年5月20日 102（e）日期1998年5月20日PCT 1996年9月26日PCT公布。公开号WO97 / 11954 日期1997年4月3日提供了制备下述通式（Ia）或（Ib）的光学活性（R） - 或（S）-1-氨基膦酸衍生物的方法，该方法包括使氨基具有通式（II）的保护的亚胺：R1-N = CHR2其中R1是二苯基甲基等，R2是烷基等，与膦酸酯在由稀土组成的不对称催化剂存在下元素 - 碱金属 - 联萘酚络合物，制备（R） - 或（S）-N-保护的1-氨基膦酸酯化合物，然后使膦酸酯化合物用氢气进行催化还原和酸性水解。还提供了新颖的中间体，以及制备由稀有元素 - 碱金属 - 萘酚络合物组成的不对称催化剂的方法。

7. 发明授权

US5847186A Process for preparing asymmetric compound by using metal complex 失效
标题翻译：使用金属络合物制备不对称化合物的方法
公开(公告)号：US5847186A
公开(公告)日：1998-12-08
申请号：US913784
申请日：1997-12-05
申请人： Masakatsu Shibasaki , Hiroaki Sasai , Takayoshi Arai
发明人： Masakatsu Shibasaki , Hiroaki Sasai , Takayoshi Arai
IPC分类号： B01J31/22 , B01J31/02 , B01J31/14 , C07B53/00 , C07B61/00 , C07C67/333 , C07C67/347 , C07C69/716 , C07C69/738 , C07F9/40 , C07F9/02 , C07C69/74
CPC分类号： C07F9/4056 , B01J31/143 , B01J31/1805 , B01J31/223 , C07B53/00 , C07C67/347 , C07F9/4006 , C07F9/4015 , C07F9/4018 , B01J2231/323 , B01J2231/341 , B01J2231/348 , B01J2531/0266 , B01J2531/11 , B01J2531/31
摘要： A process for producing an asymmetric compound using a metal complex containing no rare earth metal element is disclosed. The process affords an optically active compound having high optical purity. Optically active binaphthol having the chemical formula ##STR1## and lithium aluminum hydride are reacted, or the optically active binaphthol, a dialkyl aluminum hydride, and a base containing an alkali metal (or a base containing alkaline earth metal) are reacted to prepare a metal complex comprising optically active binaphthol, aluminum, and alkali metal (or alkaline earth metal). This metal complex can be used as a catalyst to perform an asymmetric Michael reaction, an asymmetric phosphonylation reaction, or the like, to obtain, in a high yield, an asymmetric compound having high optical purity.
摘要翻译： PCT No.PCT / KP96 / 00739 Sec。 371 1997年12月5日第 102（e）日期1997年12月5日PCT 1996年3月21日PCT公布。公开号WO96 / 29295 日本1996年9月26日公开了使用不含稀土金属元素的金属络合物制造不对称化合物的方法。该方法提供具有高光学纯度的光学活性化合物。使具有化学式“IMAGE”和氢化锂铝的光学活性联萘酚反应，或光学活性联萘酚，二烷基氢化铝和含有碱金属（或碱土金属的碱）的碱反应，制备金属络合物，其包含光学活性联萘酚，铝和碱金属（或碱土金属）。该金属络合物可用作催化剂进行不对称迈克尔反应，不对称膦酰化反应等，以高产率获得具有高光学纯度的不对称化合物。

8. 发明授权

US5336653A Catalyst for asymmetric synthesis 失效
标题翻译：不对称合成催化剂
公开(公告)号：US5336653A
公开(公告)日：1994-08-09
申请号：US970867
申请日：1992-11-03
申请人： Masakatsu Shibasaki , Hiroaki Sasai
发明人： Masakatsu Shibasaki , Hiroaki Sasai
IPC分类号： B01J31/22 , C07C201/12 , C07C205/15 , C07C205/16 , B01J31/00
CPC分类号： B01J31/223 , B01J31/0212 , B01J31/0214 , B01J2231/341 , B01J2531/0266 , B01J2531/37
摘要： The present invention provides a catalyst for asymmetric synthesis prepared from a dialkali metal salt of an optically active 2,2'-dihydroxy-1,1'-binaphthyl represented by the formula (I.sub.R) ##STR1## or the formula (I.sub.S) ##STR2## (wherein M is Li, K or Na), a lanthanum compound represented by LaX.sub.3 (X is F, Cl, Br, I, NO.sub.3 or CH.sub.3 CO.sub.2) and an alkali metal alkoxide or an alkali metal hydroxide represented by MOR or MOH (M is Li, K or Na, and R is isopropyl or t-butyl), respectively, in the presence of a water-containing solvent. The catalyst of the present invention is extremely valuable as a catalyst for asymmetric synthesis of an asymmetric nitroaldol reaction useful in the synthesis of a .beta.-hydroxynitro compound which is an important synthetic raw material for an optically active compound such as a medicine.
摘要翻译：本发明提供一种由式（1R）表示的光学活性2,2'-二羟基-1,1'-联萘的二碱金属盐制备的不对称合成催化剂（IR）或式（I ）（其中M为Li，K或Na），LaX 3（X为F，Cl，Br，I，NO 3或CH 3 CO 2）表示的镧化合物和碱金属醇盐或碱金属氢氧化物分别通过MOR或MOH（M是Li，K或Na，R是异丙基或叔丁基）。本发明的催化剂作为用于不对称合成不对称硝基醛醇反应的催化剂是非常有价值的，该反应可用于合成β-羟基硝基化合物，β-羟基硝基化合物是光学活性化合物如药物的重要合成原料。

9. 发明授权

US06677461B2 Ligands and asymmetric catalysts made by using the same 失效
标题翻译：配体和不对称催化剂通过使用它们制备
公开(公告)号：US06677461B2
公开(公告)日：2004-01-13
申请号：US10070724
申请日：2002-07-30
申请人： Masakatsu Shibasaki , Motomu Kanai , Yoshitaka Hamashima
发明人： Masakatsu Shibasaki , Motomu Kanai , Yoshitaka Hamashima
IPC分类号： C07D30910
CPC分类号： C07F9/74 , B01J31/1875 , B01J31/2226 , B01J31/223 , B01J2231/341 , B01J2531/26 , B01J2531/27 , B01J2531/28 , B01J2531/32 , B01J2531/38 , C07F7/003 , C07F9/6552 , C07F9/6596
摘要： A ligand expressed by a general formula (1) in claim 1, wherein R1, R2 and R3 denote substituting groups on aromatic rings, X is P or As, and n is 1 to 3.
摘要翻译：由权利要求1的通式（1）表示的配体，其中R 1，R 2和R 3表示芳环上的取代基，X为P或As，n为1至3。

10. 发明授权

US4762936A Bicyclo(3.3.0)Octene derivatives 失效
标题翻译：双环（3.3.0）辛烯衍生物
公开(公告)号：US4762936A
公开(公告)日：1988-08-09
申请号：US940349
申请日：1986-12-11
申请人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
发明人： Masakatsu Shibasaki , Toshiaki Mase , Mikiko Sodeoka , Yuji Ogawa
IPC分类号： C07C405/00 , C07F7/18 , C07D309/10 , C07C47/40 , C07C35/26
CPC分类号： C07F7/1856 , C07C405/0016 , C07C405/0025 , C07C405/0083 , Y02P20/55
摘要： There are disclosed a bicyclo[3.3.0]octene derivatives having the following formula: ##STR1## wherein R.sup.1 : a straight, branched or cyclic alkyl group or alkenyl group each having 5 to 10 carbon atoms;R.sup.2 and R.sup.3 : each represent a hydrogen atom or a protective group of a hydroxy group; andR.sup.4 : --CH.dbd.CH--(CH.sub.2).sub.2 --COOR.sup.5 or --CH.sub.2 R.sup.6 ; whereR.sup.5 : a hydrogen atom or an alkyl group; andR.sup.6 : a hydroxy group, an acetyloxy group or a butenyl group,and process for producing the same. These compounds and the process for producing them are available for producing a 9(0)-methano-.DELTA..sup.6 (9.alpha.)-PGI.sub.1.
摘要翻译：公开了具有下式的双环[3.3.0]辛烯衍生物：其中R 1：各自具有5-10个碳原子的直链，支链或环状烷基或烯基; R2和R3各自表示氢原子或羟基的保护基; 和R 4：-CH = CH-（CH 2）2 -COOR 5或-CH 2 R 6; 其中R5为氢原子或烷基; 和R6：羟基，乙酰氧基或丁烯基，及其制备方法。这些化合物及其制备方法可用于制备9（0） - 甲 - △DELTA 6（9α）-PGI1。

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