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    Process for preparing trans-.beta.-benzoylacrylic acid ester
    1.
    发明授权
    Process for preparing trans-.beta.-benzoylacrylic acid ester 失效
    反式β-苯甲酰丙烯酸酯的制备方法

    公开(公告)号：US4994600A

    公开(公告)日：1991-02-19

    申请号：US869782

    申请日：1986-06-02

    申请人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Yoshifumi Yanagida ,  Namito Yoshio ,  Takehisa Ohashi ,  Kiyoshi Watanabe

    发明人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Yoshifumi Yanagida ,  Namito Yoshio ,  Takehisa Ohashi ,  Kiyoshi Watanabe

    IPC分类号： C07C69/738 ,  B01J27/02 ,  B01J31/02 ,  B01J31/14 ,  C07B61/00 ,  C07C67/327

    CPC分类号： C07C67/327

    摘要： A process for preparing trans-.beta.-benzoylacrylic acid ester having the general formula (I): ##STR1## wherein R is alkyl group or aralkyl group, which comprises dealcoholizing .beta.-benzoyl-.alpha.-alkoxypropionic acid ester having the general formula (II): ##STR2## wherein R is above, in the presence of an acid catalyst to give trans-.beta.-benzoylacrylic acid ester having the general formula (I).According to the process of the present invention, the by-product (II) produced in the esterification reaction of .beta.-benzoylacrylic acid (III) with the alcohol (V) by the dehydration reaction can be converted into the compound (I) by the dealcoholization reaction in the presence of the acid catalyst and thus trans-.beta.-benzoylacrylic acid ester (I) with a high purity can be produced in an industrially advantageous manner.

    摘要翻译： 制备具有通式（I）的反式-β-苯甲酰基丙烯酸酯的方法：其中R是烷基或芳烷基，其包括使具有通式（I）的β-苯甲酰基-α-烷氧基丙酸酯脱醇 （II）：其中R在上面，在酸催化剂存在下，得到具有通式（I）的反式-β-苯甲酰基丙烯酸酯。 根据本发明的方法，通过脱水反应在β-苯甲酰基丙烯酸（III）与醇（V）的酯化反应中产生的副产物（II）可以通过 在酸催化剂存在下脱醇反应，从而可以以工业上有利的方式生产具有高纯度的反式-β-苯甲酰基丙烯酸酯（I）。

    Process for preparing optically active hydantoins
    6.
    发明授权
    Process for preparing optically active hydantoins 失效
    制备光学活性乙内酰脲的方法

    公开(公告)号：US4812406A

    公开(公告)日：1989-03-14

    申请号：US775090

    申请日：1985-09-12

    申请人： Satomi Takahashi ,  Yukio Yamada ,  Yasuyoshi Ueda ,  Yasuhiro Katayama ,  Yoshio Shimada ,  Kiyoshi Watanabe

    发明人： Satomi Takahashi ,  Yukio Yamada ,  Yasuyoshi Ueda ,  Yasuhiro Katayama ,  Yoshio Shimada ,  Kiyoshi Watanabe

    IPC分类号： C07D233/72 ,  C07D233/74 ,  C07D311/68 ,  C07D317/60 ,  C07D405/06 ,  C07D491/10 ,  C12P17/02 ,  C12P17/10 ,  C12P17/18 ,  C12P41/00 ,  C12R1/01 ,  C12R1/07 ,  C12R1/15 ,  C12R1/365 ,  C12P13/04

    CPC分类号： C07D405/06 ,  C07D233/74 ,  C07D311/68 ,  C07D317/60 ,  C07D491/10 ,  C12P17/02 ,  C12P17/10 ,  C12P17/18 ,  C12P41/009

    摘要： A process for preparing optically active hydantoins having the general formula (II): ##STR1## wherein R.sup.1 and R.sup.2, which are different from each other, are independently alkyl group, aralkyl group, aryl group, substituted alkyl group, substituted aralkyl group, or substituted aryl group, or R.sup.1 and R.sup.2 form an asymmetric cyclic compound, characterized in that one configuration of racemic N-carbamoyl-.alpha.-amino acid having the general formula (I): ##STR2## wherein R.sup.1 and R.sup.2 are as above, is enzymatically converted into the corresponding hydantoins.The present invention provides a process for an optical resolution with a high efficiency which can be used for the synthesis of (S)-6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione (USAN; Sorbinil), which is an optically active hydrantoins attracting public attention as a preventive or a remedy for the particular chronic symptoms of diabetes such as cataract and neuropathy, and (S)-.alpha.-methyl-3,4-dihydroxyphenylalanine (L-methyldopa), which is an optically active amino acid widely used as antihypertensives. Further, the present invention provides a novel finding that N-carbamoyl-.alpha.-amino acid having no hydrogen atom on its .alpha.-carbon atom can be biochemically converted into hydantoins by an enzymatic cyclization reaction.

    摘要翻译： 制备具有通式（II）的光学活性乙内酰脲的方法：其中R1和R2彼此不同，其独立地为烷基，芳烷基，芳基，取代的烷基，取代的芳烷基 基团或取代的芳基，或R 1和R 2形成不对称环状化合物，其特征在于具有通式（I）的外消旋N-氨基甲酰基-α-氨基酸的一种构型：其中R1和R2 如上所述，被酶转化成相应的乙内酰脲。 本发明提供了可用于（S）-6-氟 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮的合成的高效光学拆分方法。 （USAN; Sorbinil）是一种光学活性的水解素，引起公众的注意，作为预防或治疗糖尿病的特殊慢性症状如白内障和神经病，以及（S）-α-甲基-3,4-二羟基苯丙氨酸（L 甲基多巴），其是广泛用作抗高血压药物的光学活性氨基酸。 此外，本发明提供了一种新的发现，其α-碳原子上不具有氢原子的N-氨基甲酰基-α-氨基酸可以通过酶环化反应生物化学转化成乙内酰脲。

    Process for preparing 6-fluoro-4-chromanone using 3-(4-fluorophenoxy)propionitrile
    7.
    发明授权
    Process for preparing 6-fluoro-4-chromanone using 3-(4-fluorophenoxy)propionitrile 失效
    使用3-（4-氟苯氧基）丙腈制备6-氟-4-苯并二氢吡喃酮的方法

    公开(公告)号：US4625042A

    公开(公告)日：1986-11-25

    申请号：US752439

    申请日：1985-07-08

    申请人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Yoshio Shimada ,  Kiyoshi Watanabe

    发明人： Satomi Takahashi ,  Yasuyoshi Ueda ,  Yoshio Shimada ,  Kiyoshi Watanabe

    IPC分类号： B01J23/00 ,  B01J31/02 ,  C07B61/00 ,  C07C59/90 ,  C07C67/00 ,  C07C253/00 ,  C07C255/13 ,  C07C255/53 ,  C07D311/22 ,  C07D311/68 ,  C07C121/75

    CPC分类号： C07C255/00 ,  C07D311/22

    摘要： The present invention relates to 3-(4-fluorophenoxy)propionitrile having the formula (I): ##STR1## a process for preparing 3-(4-fluorophenoxy)propionitrile having the formula (I) which comprises reacting 4-fluorophenol and acrylonitrile in the presence of a tertiary amine, a process for preparing 6-fluoro-4-chromanone having the formula (II): ##STR2## which comprises reacting 3-(4-fluorophenoxy)propionitrile having the formula (I) with an acid, and a process for preparing 6-fluoro-4-chromanone having the formula (II) which comprises reacting 4-fluorophenol with acrylonitrile in the presence of a catalyst to give 3-(4-fluorophenoxy)propionitrile having the formula (I), which is then reacted with an acid. 6-Fluoro-4-chromanone is an important intermediate for the synthesis of (S)-2,3-dihydro-6-fluoro-spiro[4H-1-benzopyran-4,4'-imidazolidine]-2',5'dione (USAN: sorbinil).

    摘要翻译： 本发明涉及具有式（I）的3-（4-氟苯氧基）丙腈：（I）制备具有式（I）的3-（4-氟苯氧基）丙腈的方法，该方法包括使4-氟苯酚 （II）的6-氟-4-苯并二氢吡喃酮的制备方法：包括使具有式（I）的3-（4-氟苯氧基）丙腈与式 ）和用于制备具有式（II）的6-氟-4-苯并二氢吡喃酮的方法，其包括在催化剂存在下使4-氟苯酚与丙烯腈反应，得到具有式（II）的3-（4-氟苯氧基）丙腈 （I），然后与酸反应。 6-氟-4-苯并二氢吡喃酮是合成（S）-2,3-二氢-6-氟 - 螺[4H-1-苯并吡喃-4,4'-咪唑烷] -2'，5' 二酮（USAN：sorbinil）。

    Process for preparing 4-acetoxy-3-hydroxyethylazetidin-2-one derivatives
    8.
    发明授权
    Process for preparing 4-acetoxy-3-hydroxyethylazetidin-2-one derivatives 失效

    公开(公告)号：US4914199A

    公开(公告)日：1990-04-03

    申请号：US156873

    申请日：1988-02-18

    申请人： Isao Sada ,  Kazunori Kan ,  Noboru Ueyama ,  Shingo Matsumoto ,  Takehisa Ohashi ,  Kiyoshi Watanabe

    发明人： Isao Sada ,  Kazunori Kan ,  Noboru Ueyama ,  Shingo Matsumoto ,  Takehisa Ohashi ,  Kiyoshi Watanabe

    IPC分类号： C07D205/08 ,  C07F7/18

    CPC分类号： C07F7/186 ,  C07D205/08 ,  Y02P20/55

    摘要： A process for preparing a 4-acetoxy-3-hydroxyethylazetidin-2-one derivative having the formula (II): ##STR1## wherein R.sup.1 is a protective group for the hydroxyl group, which comprises reactig a .beta.-lactam compound having the formula (I): ##STR2## wherein R.sup.1 is as difined above and R.sup.2, R.sup.3 and R.sup.4 are the same or different and each is a lower alkyl group having 1 to 4 carbon atoms or an aralkyl group, with acetic anhydride in the presence of a base and a catalyst selected from the group consisting of an organic strong acid, a mineral acid, a Lewis acid, a halogenated acyl compound having the formula (IV):R.sup.8 --CO--X (IV)wherein R.sup.8 is an alkyl group, an aralkyl group or phenyl group and X is a halogen atom, a halogenated sulfonyl compound having the formula (V):R.sup.9 --SO.sub.2 --X (V)wherein R.sup.9 is an alkyl group, an aralkyl group or phenyl group and X is a halogen atom, and a compound having the formula (VI):(R.sup.10).sub.4-n --Si(X').sub.n (VI)wherein R.sup.10 is a lower alkyl group having 1 to 6 carbon atoms or phenyl group, X' is a halogen atom or CF.sub.3 SO.sub.2 O group and n is an integer of 1 to 4. According to the present invention, there can be obtained 4-acetoxy-3-hydroxyethylazetidin-2-one derivatives, which are useful intermediates for preparing carbapenem .beta.-lactam antibiotics, in high yield.

    Method for producing optically active glycol derivatives
    9.
    发明授权
    Method for producing optically active glycol derivatives 失效
    光学活性二醇衍生物的制备方法

    公开(公告)号：US4745066A

    公开(公告)日：1988-05-17

    申请号：US846766

    申请日：1986-04-01

    申请人： Shigeki Hamaguchi ,  Takehisa Ohashi ,  Kiyoshi Watanabe

    发明人： Shigeki Hamaguchi ,  Takehisa Ohashi ,  Kiyoshi Watanabe

    IPC分类号： C07B31/00 ,  C07C67/00 ,  C07C301/00 ,  C07C303/22 ,  C07C309/72 ,  C12P11/00 ,  C12P41/00 ,  C12R1/01 ,  C12R1/38 ,  C12R1/66 ,  C12R1/785 ,  C12R1/845

    CPC分类号： C12P41/004 ,  C07C309/00 ,  C12P11/00

    摘要： A method for producing optically active glycol derivatives by biochemical resolution which comprises contacting a racemic ester of the general formula 1 ##STR1## (wherein R.sub.1 is an aliphatic hydrocarbon group of 1 to 16 carbon atoms, R.sub.2 is an aliphatic hydrocarbon group of 1 to 8 carbon atoms, and R.sub.3 is an aromatic hydrocarbon group such as phenyl, tolyl or naphtyl) with a microorganism- or animal organ-derived enzyme having stereoselective hydrolytic activity to asymmetrically hydrolyze said racemic ester of general formula 1 to produce an optically active alcohol of general formula 2* ##STR2## (wherein R.sub.1 and R.sub.3 have the same meanings as defined above) and an unreacted ester of the general formula 1* ##STR3## (wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as defined hereinbefore), separating the optically active compounds from each other, hydrolyzing said ester of general formula 1* to give an optically active glycol derivative which is antipodal to the alcohol of general formula 2* and, then, isolating the same optically active glycol derivative. The invention provides a method for producing optically active glycol derivatives, which is expedient, does not require costly reagents and is suited to commercial scale production.

    摘要翻译： 一种通过生物化学拆分制备光学活性二醇衍生物的方法，其包括使通式1的外消旋酯1（其中R 1是1至16个碳原子的脂族烃基，R 2是1的脂族烃基， 8个碳原子，并且R 3是芳族烃基如苯基，甲苯基或萘基）与具有立体选择性水解活性的微生物或动物器官衍生的酶不对称地水解所述通式1的外消旋酯以产生光学活性的醇 通式2 * 2 *（其中R 1和R 3具有与上述相同的含义）和通式1 *未反应的酯*（其中R 1，R 2和R 3具有与定义相同的含义） 将光学活性化合物彼此分离，水解所述通式1 *的酯，得到对通式为醇的对映体的光学活性二醇衍生物 2 *，然后分离相同的光学活性二醇衍生物。 本发明提供了一种制备光学活性二醇衍生物的方法，这是有利的，不需要昂贵的试剂并且适于商业规模生产。

    Process for preparation of optically active N-mercaptoalkanoylamino acids
    10.
    发明授权
    Process for preparation of optically active N-mercaptoalkanoylamino acids 失效
    光学活性N-巯基烷酰氨基酸的制备方法

    公开(公告)号：US4371699A

    公开(公告)日：1983-02-01

    申请号：US214780

    申请日：1980-12-09

    申请人： Takehisa Ohashi ,  Masami Shimazaki ,  Kazunori Kan ,  Hideo Kondo ,  Kiyoshi Watanabe

    发明人： Takehisa Ohashi ,  Masami Shimazaki ,  Kazunori Kan ,  Hideo Kondo ,  Kiyoshi Watanabe

    IPC分类号： C07C51/60 ,  C07D207/16 ,  C07D211/60 ,  C07D277/06 ,  C07K5/078

    CPC分类号： C07K5/06165 ,  C07C51/60 ,  C07D207/16 ,  C07D211/60 ,  C07D277/06

    摘要： A process is disclosed wherein an optically active N-mercaptoalkanoylamino acid is prepared by(1) reacting an optically active .beta.-hydroxyalkanoic acid, with a halogenating reagent to prepare an optically active .beta.-haloalkanoyl halide(2) reacting the .beta.-haloalkanoyl halide with an amino acid to produce an optically active N-.beta.-haloalkanoylamino acid and(3) reacting the N-.beta.-haloalkanoylamino acid with a reagent capable of converting the halogen into the thiol group, the configuration of the formulas (II), (III), (IV), (V), and (VI) being retained in all the optically active compounds throughout the process to prepare the compound represented by formula (I). The product of the present invention, for example, N-(3-mercapto-2-D-methylpropanoyl)-L-proline inhibits the enzymatic conversion of angiotensin I into angiotensin II and therefore is useful for relieving angiotensin-related hypertension.

    摘要翻译： 公开了一种方法，其中光学活性N-巯基烷酰基氨基酸通过（1）使光学活性β-羟基链烷酸与卤化试剂反应制备光学活性β-卤代烷酰基卤化物（2）使β-卤代烷酰卤与 氨基酸以产生光学活性的N-β-卤代烷酰基氨基酸和（3）使N-β-卤代烷酰基氨基酸与能够将卤素转化成硫醇基团的试剂反应，式（II），（III ），（IV），（V）和（VI）在整个过程中保留在所有光学活性化合物中以制备由式（I）表示的化合物。 本发明的产物，例如N-（3-巯基-2-D-甲基丙酰基）-L-脯氨酸抑制血管紧张素I的酶促转化为血管紧张素II，因此可用于缓解血管紧张素相关的高血压。