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1. 发明申请

US20060194867A1 PROCESS FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES 失效
标题翻译：制备ATORVASTATIN和中间体的方法
公开(公告)号：US20060194867A1
公开(公告)日：2006-08-31
申请号：US11099624
申请日：2005-04-06
申请人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/401 , C07D207/34
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基 ] -3-羟基-1-戊酸，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基） 3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

2. 发明申请

US20050004625A1 Treatment of degenerative retinal disease via electrical stimulation of surface structures 审中-公开
标题翻译：通过电刺激表面结构治疗退行性视网膜疾病
公开(公告)号：US20050004625A1
公开(公告)日：2005-01-06
申请号：US10863519
申请日：2004-06-09
申请人： Alan Chow
发明人： Alan Chow
IPC分类号： A61F9/00 , A61N1/05 , A61N1/32 , A61N1/36 , A61N1/18
CPC分类号： A61N1/0543 , A61F9/0017 , A61N1/326 , A61N1/36046
摘要： To provide indirect electrical stimulation for treatment of degenerative retinal diseases, such stimulation is applied to surface structures of the eye. A source of an electrical stimulation signal is coupled to a first electrode configured for contact with a first internal surface structure of an eyeball. A second electrode, which may be configured either for contact with an internal surface structure or an external surface structure of the eyeball, is also coupled to the source. The source of the electrical stimulation signal may be implemented internal to a body of a patient, external to the body or through a combined internal/external approach. The first and second electrodes are preferably arranged such that the circuit created by the source, electrodes and intervening biological tissue provides trans-retinal electrical stimulation to thereby effect treatment.
摘要翻译：为了提供间接电刺激治疗退行性视网膜疾病，这种刺激被应用于眼睛的表面结构。电刺激信号的源耦合到构造成与眼球的第一内表面结构接触的第一电极。可以被配置为与眼球的内表面结构或外表面结构接触的第二电极也耦合到源。电刺激信号的源可以在身体外部或通过组合的内部/外部方法在患者的身体内部实现。第一和第二电极优选地布置成使得由源，电极和中间生物组织产生的电路提供视网膜电刺激，从而进行治疗。

3. 发明授权

US07429613B2 Process for the preparation of atorvastatin and intermediates 失效
标题翻译：制备阿托伐他汀和中间体的方法
公开(公告)号：US07429613B2
公开(公告)日：2008-09-30
申请号：US11487500
申请日：2006-07-17
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/4025 , C07D207/327
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基 ] -3-羟基-1-戊酸，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基） 3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

4. 发明申请

US20060252816A1 Process for the preparation of atorvastatin and intermediates 失效
公开(公告)号：US20060252816A1
公开(公告)日：2006-11-09
申请号：US11487500
申请日：2006-07-17
申请人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Guntoori , Yajun Zhao , Aaron Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/401
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.

5. 发明申请

US20060142818A1 Methods for improving damaged retinal cell function 审中-公开
公开(公告)号：US20060142818A1
公开(公告)日：2006-06-29
申请号：US11301352
申请日：2005-12-12
申请人： Alan Chow , Vincent Chow
发明人： Alan Chow , Vincent Chow
IPC分类号： A61N1/18
CPC分类号： A61F9/0017 , A61N1/0543 , A61N1/36046
摘要： Methods of using electrical stimulation by itself or in conjunction with growth factors to treat and prevent visual loss due to choroidal, retinal pigment epithelial and/or neuroretinal cell degeneration and dysfunction are presented.

6. 发明授权

US06907338B2 Controller and control method for injection using function map 失效
标题翻译：使用功能图进行注射的控制器和控制方法
公开(公告)号：US06907338B2
公开(公告)日：2005-06-14
申请号：US10388248
申请日：2003-03-13
申请人： Jason Paul Frankl , Alan Chow , Vidya Shankar Somasundaram , Edward Thomas Williams
发明人： Jason Paul Frankl , Alan Chow , Vidya Shankar Somasundaram , Edward Thomas Williams
IPC分类号： F02D41/24 , F02D41/30
CPC分类号： F02D41/2422 , F02D41/2416 , F02D41/30
摘要： A method of controlling an injector or the like suitable for use in an internal combustion engine, includes providing a first data map having a plurality of first data map points, each of the first data map points representing a first data map output value, and providing a function map comprising a second data map having a plurality of second data map points, each corresponding to a respective one of the first data map points, and wherein the second data map is divided into at least a first-type data map region containing second data map points representing second data map output values only of a first type and a second-type data map region containing second data map points representing second data map output values only of a second type, wherein a portion of the second data map defines a hysteresis region. The method also includes determining an operating point on an operating path within the second data map in dependence upon first and second engine operating parameters and determining a control function for the injector based on a first data map output value determined from the first data map and the second data map output value determined from the second data map, in dependence upon whether the operating point in the second data map lies in a part of the first-type data map region which is outside the hysteresis region, or whether the operating point in the second data map lies in a part of the first-type data map region which is within the hysteresis region.
摘要翻译：一种控制适用于内燃机的喷射器等的方法，包括提供具有多个第一数据映射点的第一数据图，每个第一数据图点表示第一数据图输出值，并提供功能图，包括具有多个第二数据映射点的第二数据图，每个第二数据映射点对应于第一数据映射点中的相应一个，并且其中第二数据映射被划分为至少第一类型数据映射区域，其包含第二数据映射点数据映射点表示仅第一类型和第二类型数据映射区域的第二数据映射输出值，该第二数据映射区域包含仅表示第二类型的第二数据映射输出值的第二数据映射点，其中第二数据映射的一部分定义了滞后地区。该方法还包括根据第一和第二发动机操作参数来确定第二数据图中的操作路径上的操作点，并且基于从第一数据图和第一数据图确定的第一数据图输出值确定喷射器的控制功能第二数据图输出值根据第二数据图中的工作点是否位于滞后区域外的第一类型数据图区域的一部分，或者是否位于第二数据图中的工作点第二数据图位于滞后区域内的第一类型数据图区域的一部分。

7. 发明申请

US20050033202A1 Mechanically activated objects for treatment of degenerative retinal disease 审中-公开
标题翻译：机械活化物体治疗退行性视网膜疾病
公开(公告)号：US20050033202A1
公开(公告)日：2005-02-10
申请号：US10822437
申请日：2004-04-12
申请人： Alan Chow , George McLean , Vincent Chow , Jay Cech , Christopher Bonner , Vladimir Gelfandbein
发明人： Alan Chow , George McLean , Vincent Chow , Jay Cech , Christopher Bonner , Vladimir Gelfandbein
IPC分类号： A61H1/00 , A61H5/00 , A61N1/05 , A61N1/36 , A61N2/06 , A61N2/12
CPC分类号： A61N1/36046 , A61H5/00 , A61N1/0543 , A61N2/06 , A61N2/12
摘要： Mechanically activated objects or devices for use in treating degenerative retinal diseases are provided. Such devices apply mechanical forces to tissues of an eye to effectuate treatment and are configured for chronic implantation (thereby applying chronic stimulation/irritation) in or on the eye. The devices may be configured for contact with a retina of the eye, preferably positioned in a subretinal space. Various embodiments comprise a moving member configured for chronic contact with at least a portion of the eye, which moving member is activated by an actuator. In some embodiments, the actuator may be distally located relative to the moving member. Alternatively, the moving member may be supported by a body member that, optionally, also supports the actuator.
摘要翻译：提供用于治疗退行性视网膜疾病的机械活化物体或装置。这样的装置将机械力施加到眼睛的组织以实现治疗，并且被配置为在眼睛中或眼睛上进行慢性植入（从而施加慢性刺激/刺激）。所述装置可以被配置为与眼睛的视网膜接触，优选地定位在视网膜下空间中。各种实施例包括构造成用于与眼睛的至少一部分慢性接触的移动构件，该移动构件由致动器致动。在一些实施例中，致动器可以相对于移动构件向远侧定位。或者，移动构件可以由主体构件支撑，其可选地还支撑致动器。

8. 发明授权

US07812179B2 Process for the preparation of atorvastatin and intermediates 失效
标题翻译：制备阿托伐他汀和中间体的方法
公开(公告)号：US07812179B2
公开(公告)日：2010-10-12
申请号：US12222690
申请日：2008-08-14
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： C07D207/333
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基 ] -3-羟基-1-戊酸，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基） 3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

9. 发明授权

US07112604B2 Process for the preparation of Atorvastatin and intermediates 失效
标题翻译：阿托伐他汀和中间体的制备方法
公开(公告)号：US07112604B2
公开(公告)日：2006-09-26
申请号：US11099624
申请日：2005-04-06
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： A61K31/4025 , C07D207/327
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基 ] -3-羟基-1-戊酸，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐，得到对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基） 3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

10. 发明申请

US20090131683A1 Process for the preparation of atorvastatin and intermediates 失效
标题翻译：制备阿托伐他汀和中间体的方法
公开(公告)号：US20090131683A1
公开(公告)日：2009-05-21
申请号：US12222690
申请日：2008-08-14
申请人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
发明人： Fan Wang , Daqing Che , Bhaskar Reddy Guntoori , Yajun Zhao , Aaron C. Kinsman , Jody Faught , Alan Chow
IPC分类号： C07D207/333
CPC分类号： C07D207/34
摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting the aldehyde 1 with the enolate form of (S)-2-hydroxy-1,2,2-triphenylethyl acetate substituent in a chelating co-solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (S)-2-hydroxy-1,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the carboxylic acid 7; (c) treating the acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free base derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, R-substituted ester 9 and atorvastatin calcium 6, wherein R is a C1 to C6 alkyl, C6 to C9 aryl or C7 to C10 aralkyl.
摘要翻译：提供了制备（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9，其包含：（a）使醛1与烯醇化形式的（S）-2-羟基-1,2,2-三苯基乙基乙酸酯取代基在螯合助溶剂中; （b）（R，S）-5- [2-（4-氟苯基）-5-（1-甲基乙基）-3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基 ] -3-羟基-1-戊酸，（S）-2-羟基-1,2,2-三苯基乙酯（2a和2b），使用碱，优选碱金属碱，优选在溶剂中形成羧酸酸7; （c）用手性碱处理酸7以形成盐并纯化该盐以获得对映体富集的（R）-7手性碱盐; （d）（R）-7手性碱盐或衍生自（R）-7的游离碱的烷基化，形成（R）-5- [2-（4-氟苯基）-5-（1-甲基乙基） - 3-苯基-4 - [（苯基氨基）羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸，R-取代的酯9和阿托伐他汀钙6，其中R是C1 C6烷基，C6〜C9芳基或C7〜C10芳烷基。

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