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1. 发明专利

IL277419D0 Kv7 channel activators compositions and methods of use 未知
公开(公告)号：IL277419D0
公开(公告)日：2020-11-30
申请号：IL27741920
申请日：2020-09-16
申请人： KNOPP BIOSCIENCES LLC , MICHAEL E BOZIK , SCOTT S HARRIED , LYNN RESNICK , GEORGE T TOPALOV , JUSTIN K BELARDI , CHARLES A FLENTGE , DAVID A MARESKA , JAMES S HALE
发明人： MICHAEL E BOZIK , SCOTT S HARRIED , LYNN RESNICK , GEORGE T TOPALOV , JUSTIN K BELARDI , CHARLES A FLENTGE , DAVID A MARESKA , JAMES S HALE
摘要： Provided herein are optionally substituted benzoimidazol-1,2-yl amides, pharmaceutical compositions comprising a therapeutically effective amount of such compounds and a pharmaceutically acceptable excipient, and methods of treating Kv7 associated diseases, such as, epilepsy, amyotrophic lateral sclerosis, various types of pain, hyperexcitability, a dyskinesia, dystonia, mania and tinnitus with such compounds and pharmaceutical compositions.

2. 发明授权

US07399778B2 Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole 失效
标题翻译：含有唑类的β-淀粉样蛋白产生的杂环磺酰胺抑制剂
公开(公告)号：US07399778B2
公开(公告)日：2008-07-15
申请号：US11035005
申请日：2005-01-13
申请人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
发明人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： A61K31/416 , C07D231/12 , C07D409/12
摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译：提供了可用于降低β淀粉样蛋白水平的化合物。化合物具有式Ia的结构：其中R 1是低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2， / 5> 5

3. 发明申请

US20070117794A1 Methods of treatment using oxytocin receptor agonists 审中-公开
标题翻译：使用催产素受体激动剂治疗的方法
公开(公告)号：US20070117794A1
公开(公告)日：2007-05-24
申请号：US11584995
申请日：2006-10-23
申请人： Zia Rahman , Lynn Resnick , Sharon Rosenzweig-Lipson , Robert Ring
发明人： Zia Rahman , Lynn Resnick , Sharon Rosenzweig-Lipson , Robert Ring
IPC分类号： A61K31/551
CPC分类号： A61K31/551 , C07D487/04 , C07D495/14
摘要： Methods for treating and preventing anxiety, anxiety-related disorders, schizophrenia and schizophrenia-related disorders are described herein wherein said methods comprise the administration of oxytocin receptor agonists.
摘要翻译：治疗和预防焦虑，焦虑相关疾病，精神分裂症和精神分裂症相关疾病的方法在本文中描述，其中所述方法包括施用催产素受体激动剂。

4. 发明申请

US20080249150A1 HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION CONTAINING AN AZOLE 失效
标题翻译：含有氨基酸的淀粉酶生产的杂环磺酰胺抑制剂
公开(公告)号：US20080249150A1
公开(公告)日：2008-10-09
申请号：US12142306
申请日：2008-06-19
申请人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
发明人： Lynn Resnick , Donna M. Huryn , Joan E. Sabalski , Joshua D. Berkowitz , Anthony Frank Kreft , Dennis Martin Kubrak , Thomas Joseph Caggiano , Koi Michele Morris
IPC分类号： A61K31/4196 , C07D409/02 , A61K31/415 , A61P25/28 , C07D231/12
CPC分类号： A61K31/416 , C07D231/12 , C07D409/12
摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.
摘要翻译：提供了可用于降低β淀粉样蛋白水平的化合物。化合物具有式Ia的结构：其中R 1是低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2， / 5> 5

5. 发明申请

US20070254929A1 Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
标题翻译：含有氟和三氟烷基的杂环磺酰胺抑制剂β淀粉样蛋白产生及其衍生物
公开(公告)号：US20070254929A1
公开(公告)日：2007-11-01
申请号：US11818630
申请日：2007-06-15
申请人： Anthony Kreft , Lynn Resnick , Scott Mayer , George Diamantidis , Derek Cole , Boyd Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco Galante
发明人： Anthony Kreft , Lynn Resnick , Scott Mayer , George Diamantidis , Derek Cole , Boyd Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco Galante
IPC分类号： A61K31/433 , A61P25/00 , C07D285/08
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR 8或C（OH）R 1 R 2 2; R 1和R 2均为氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R 3是氢或任选取代的低级烷基; R 4是（CF 3）n烷基，（CF 3 N）N（S）（取代的烷基），（CF 3）n烷基苯基，（CF 3）n烷基（取代的苯基）或（C 3 -C 6）烷基（F）环烷基; n = 1-3; 当Y-C时，R 5是氢，卤素，CF 3 O，与Y稠合的二烯，或Y-C时与Y稠合的取代的二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R 6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 和R 8是低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

6. 发明授权

US06657070B2 Production of chirally pure &agr;-amino acids and N-sulfonyl &agr;-amino acids 失效
标题翻译：手性纯α-氨基酸和N-磺酰基α-氨基酸的生产
公开(公告)号：US06657070B2
公开(公告)日：2003-12-02
申请号：US10166896
申请日：2002-06-11
申请人： Lynn Resnick
发明人： Lynn Resnick
IPC分类号： C07D33332
CPC分类号： C07D307/64 , C07D333/34 , C07D409/12
摘要： Methods for production of chirally pure &agr;-amino acids and N-sulfonyl &agr;-amino acids are described. An aldehyde and a cyanide salt are reacted with an &agr;-methylbenzylamine to afford product. The product reacts with a strong acid, neutralized, and extracted. The resulting product is hydrolyzed to provide a product which is dissolved in a strong acid to provide a salt of a chirally pure &agr;-amino acid, which is reacted to provide the chirally pure &agr;-amino acid. Another method involves mixing ephedrine hemihydrate and an N-sulfonyl &agr;-ethylnorvaline in ethanol at a molar ratio of 1:1; heating the mixture to dissolve the solids; cooling to allow formation of a precipitate; washing with an organic solvent to give diastereomeric salt; recrystallizing the salt; dissolving the recrystallized salt in an organic solvent and strong aqueous acid, separating the layers; washing the organic extract; drying and concentrating to provide chirally pure N-sulfonyl &agr;-amino acid.
摘要翻译：描述了生产手性纯α-氨基酸和N-磺酰基α-氨基酸的方法。使醛和氰化物盐与α-甲基苄胺反应得到产物。产物与强酸反应，中和并萃取。将所得产物水解以提供溶解在强酸中以产生手性纯的α-氨基酸的盐的产物，其被反应以提供手性纯的α-氨基酸。另一种方法包括以摩尔比1:1混合乙醇中的麻黄碱半水合物和N-磺酰基α-乙基缬氨酸; 加热混合物以溶解固体; 冷却以形成沉淀物; 用有机溶剂洗涤得到非对映体盐; 重结晶盐; 将重结晶盐溶解在有机溶剂和强酸性水溶液中，分离各层; 洗涤有机提取物; 干燥和浓缩以提供手性纯的N-磺酰基α-氨基酸。

7. 发明申请

US20090227667A1 FLUORO- AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF 失效
标题翻译：含氟和含三氟甲磺酸的苯甲酰胺酰胺抑制剂的制备及其衍生物
公开(公告)号：US20090227667A1
公开(公告)日：2009-09-10
申请号：US12435442
申请日：2009-05-05
申请人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K31/381 , C07D333/34 , C07D333/62
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F）n环烷基; n = 1-3; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

8. 发明授权

US07547725B2 Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
标题翻译： β-淀粉样蛋白产生的含氟和三氟烷基的杂环磺酰胺抑制剂及其衍生物
公开(公告)号：US07547725B2
公开(公告)日：2009-06-16
申请号：US11818630
申请日：2007-06-15
申请人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K31/381 , C07D333/10 , C07D333/34
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substituted alkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substituted phenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F） n = 1-3; 当Y-C或Y-C与Y稠合时，R 5为氢，卤素，CF 3，二烯稠合至Y; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

9. 发明授权

US07300951B2 Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
标题翻译： β-淀粉样蛋白产生的含氟和三氟烷基的杂环磺酰胺抑制剂及其衍生物
公开(公告)号：US07300951B2
公开(公告)日：2007-11-27
申请号：US10810517
申请日：2004-03-26
申请人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K31/381 , C07D333/10 , C07D333/34
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, CON, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）的化合物，其中T是CHO，CON或C（OH）R 1 R 2 R 2; R 1和R 2均为氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R 3是氢或任选取代的低级烷基; R 4是（CF 3）n烷基，（CF 3 N）N（S）（取代的烷基），（CF 3）n烷基苯基，（CF 3）n烷基（取代的苯基）或（C 3 -C 6）烷基（F）环烷基; n = 1-3; 当Y-C时，R 5是氢，卤素，CF 3 O，与Y稠合的二烯，或Y-C时与Y稠合的取代的二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R 6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 和R 8是低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

10. 发明授权

US06800764B2 Process for the synthesis of chirally pure beta-amino-alcohols 失效
标题翻译：手性纯合β-氨基醇的合成方法
公开(公告)号：US06800764B2
公开(公告)日：2004-10-05
申请号：US10304322
申请日：2002-11-26
申请人： Anthony Frank Kreft , Madelene Miyoko Antane , Derek Cecil Cole , Dennis Martin Kubrak , Lynn Resnick , Joseph Raymond Stock , Zheng Wang
发明人： Anthony Frank Kreft , Madelene Miyoko Antane , Derek Cecil Cole , Dennis Martin Kubrak , Lynn Resnick , Joseph Raymond Stock , Zheng Wang
IPC分类号： C07D33332
CPC分类号： C07C215/20 , C07B2200/07 , C07C215/08 , C07C215/24 , C07C215/28 , C07C215/56 , C07C229/08 , C07C229/28 , C07C229/30 , C07C229/36 , C07C247/12 , C07C323/63 , C07D263/26 , C07D333/34
摘要： A process is provided for preparing chirally pure S-enantiomers of &agr;-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an &agr;-azido acid; h) reducing the &agr;-azido acid to the &agr;-amino acid; and i) recrystallizing the &agr;-amino acid to the chirally pure &agr;-amino acid. A process is also provided for preparing chirally pure S-enantiomers of &bgr;-amino alcohols further comprising the steps of reducing the crude &agr;-amino acid to the &bgr;-amino alcohol and recrystallizing the &bgr;-amino alcohol to the chirally pure &bgr;-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl &bgr;-amino alcohols further comprising the steps of sulfonylating the &bgr;-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl &bgr;-amino alcohols.
摘要翻译：提供了一种用于制备α-氨基酸的手性纯的S-对映异构体的方法，包括以下步骤：a）由式（R）2CH（CH 2）n CH 2 X的烷基卤制备有机金属试剂; b）将有机金属试剂加入到二氧化碳中，得到羧酸; c）在叔胺碱存在下用酰氯，三氯化磷，酸酐或亚硫酰氯活化羧酸; d）使步骤c）的产物与S-4-苄基-2-恶唑烷酮的碱金属盐反应; e）用强非亲核碱处理步骤d）的产物以形成烯醇化物阴离子; f）用2,4,6-三异丙基苯磺酰叠氮化物捕获烯醇化阴离子，得到恶唑烷酮叠氮化物; g）用碱水溶液水解恶唑烷酮叠氮化物，得到α-叠氮基; h）将α-叠氮基还原成α-氨基酸; 和i）将α-氨基酸重结晶至手性纯的α-氨基酸。还提供了制备β-氨基醇的手性纯的S-对映异构体的方法，该方法还包括将β-氨基酸的粗α-氨基酸还原成β-氨基醇，并将β-氨基醇重结晶至手性纯的β-氨基醇。还提供了制备N-磺酰基β-氨基醇的手性纯S对映异构体的方法，其还包括用5-氯 - 噻吩-2-磺酰卤磺酰化β-氨基醇的步骤; 并重结晶得到手性纯的N-磺酰基β-氨基醇。

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