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227 条记录 (耗时 0.039 秒)

    Processes for producing .alpha.-halo ketones, .alpha.-halohydrins and epoxides
    1.
    发明授权
    Processes for producing .alpha.-halo ketones, .alpha.-halohydrins and epoxides 失效
    制备α-卤代酮，α-卤代醇和环氧化物的方法

    公开(公告)号：US5929284A

    公开(公告)日：1999-07-27

    申请号：US722102

    申请日：1996-12-18

    申请人： Akira Nishiyama ,  Tadashi Sugawa ,  Hajime Manabe ,  Kenji Inoue ,  Noritaka Yoshida

    发明人： Akira Nishiyama ,  Tadashi Sugawa ,  Hajime Manabe ,  Kenji Inoue ,  Noritaka Yoshida

    IPC分类号： C07C29/143 ,  C07C45/48 ,  C07C269/06 ,  C07C319/20 ,  C07C323/43 ,  C07D303/36 ,  C07C45/00

    CPC分类号： C07D303/36 ,  C07C269/06 ,  C07C29/143 ,  C07C319/20 ,  C07C45/48

    摘要： Processes for efficiently producing .alpha.-halo ketones, .alpha.-halohydrins and epoxides on an industrial scale. The prosesses include one for producing an .alpha.-halo ketone of general formula (3) by decarboxylating a product of reaction between a carboxilic acid derivative of general formula (1) and a metal enolate prepared from an .alpha.-haloacetic acid of general formula (2) or an acceptable salt thereof, one for producing an by reducing the .alpha.-halo ketone (3), and one for producing an epoxide (13) by treating the .alpha.-halohydrin (11) with a base to effect ring closure. The above prosesses are particularly suitable for producing optically active .alpha.-halo ketones, .alpha.-halohydrins and epoxides from the corresponding .alpha.-amino acid derivatives. ##STR1##

    摘要翻译： PCT No.PCT / JP96 / 00212 Sec。 371日期：1996年12月18日 102（e）1996年12月18日日期PCT 1996年2月2日PCT PCT。 第WO96 / 23756号公报 日期1996年8月8日工业规模高效生产α-卤代酮，α-卤代醇和环氧化物的方法。 前药包括通过使通式（1）的羧酸衍生物与由通式（2）的α-卤代乙酸制备的金属烯醇化物脱羧的方法来制备通式（3）的α-卤代酮， ）或其可接受的盐，其中通过用碱来还原α-卤代酮（3）和通过用碱处理α-卤代醇（11）来制备环氧化物（13）来制备，以实现闭环。 上述产品特别适用于从相应的α-氨基酸衍生物制备光学活性的α-卤代酮，α-卤代醇和环氧化物。

    Process for preparing optically active alcoholic compounds
    6.
    发明授权
    Process for preparing optically active alcoholic compounds 失效
    光学活性醇类化合物的制备方法

    公开(公告)号：US06187966B1

    公开(公告)日：2001-02-13

    申请号：US09011176

    申请日：1999-07-15

    申请人： Tadashi Sugawa ,  Kenji Inoue ,  Kazunori Kan

    发明人： Tadashi Sugawa ,  Kenji Inoue ,  Kazunori Kan

    IPC分类号： C07C3346

    CPC分类号： C07C29/143 ,  C07B2200/07 ,  C07C33/20

    摘要： A process for preparing optically active alcoholic compounds wherein a carbonyl compound is assymmetrically reduced in an economical and practical manner. The process comprises treating a prochiral carbonyl compound represented by the general formula (1) with an optically active organoaluminum compound represented by the general formula (2) to conduct asymmetric reduction, thereby preparing an optically active alcoholic compound represented by the general formula (3).

    摘要翻译： 一种制备光学活性醇化合物的方法，其中羰基化合物以经济和实用的方式不对称还原。该方法包括用通式（1）表示的光学活性有机铝化合物处理由通式（1）表示的前手性羰基化合物 2）进行不对称还原，由此制备由通式（3）表示的光学活性醇化合物。

    Process for production of 3-(3-pyridyl)-1-propanol derivatives
    8.
    发明授权
    Process for production of 3-(3-pyridyl)-1-propanol derivatives 失效
    3-（3-吡啶基）-1-丙醇衍生物的制备方法

    公开(公告)号：US06388086B1

    公开(公告)日：2002-05-14

    申请号：US09631678

    申请日：2000-08-02

    申请人： Akira Nishiyama ,  Kazumi Okuro ,  Kenji Inoue

    发明人： Akira Nishiyama ,  Kazumi Okuro ,  Kenji Inoue

    IPC分类号： C07D21330

    CPC分类号： C07D213/30

    摘要： A process for producing a 3-(3-pyridyl)-1-propanol derivative of use as a pharmaceutical intermediate expediently with an inexpensive material is provided. The process is concerned with a 3-(3-pyridyl)-1-propanol derivative (3): in the formula, R1 represents an alkyl group of 1 to 20 carbon atoms, aryl group of 6 to 20 carbon atoms or aralkyl group of 7 to 20 carbon atoms, which may be substituted, and comprises reacting a 3-methylpyridine with a strong base to prepare a 3-methylpyridine metal (1): in the formula, M represents lithium, sodium, potassium or a magnesium halide, where the halide is chloride or bromide, and then reacting said metal salt with an epoxy compound (2):

    摘要翻译： 提供了以便宜的材料制备用作药物中间体的3-（3-吡啶基）-1-丙醇衍生物的方法。 该方法涉及3-（3-吡啶基）-1-丙醇衍生物（3）：式中，R1表示碳原子数为1〜20的烷基，碳原子数为6〜20的芳基或芳烷基 可以被取代的7至20个碳原子，并且使3-甲基吡啶与强碱反应以制备3-甲基吡啶金属（1）：在该式中，M表示锂，钠，钾或卤化镁，其中 卤化物是氯化物或溴化物，然后使所述金属盐与环氧化合物（2）反应：

    Process for the preparation of 5-hydroxy-3-oxopentanoic acid derivatives
    9.
    再颁专利
    Process for the preparation of 5-hydroxy-3-oxopentanoic acid derivatives 有权

    公开(公告)号：USRE39333E1

    公开(公告)日：2006-10-10

    申请号：US10705665

    申请日：2000-06-02

    申请人： Akira Nishiyama ,  Kenji Inoue

    发明人： Akira Nishiyama ,  Kenji Inoue

    IPC分类号： C07C69/66 ,  C07C59/185

    CPC分类号： C12P7/62 ,  C07B2200/07 ,  C07C67/343 ,  C07C253/30 ,  C07D319/06 ,  C07C69/716 ,  C07C255/21 ,  C07C69/738

    摘要： This invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid, a useful pharmaceutical intermediate, easily from a readily available, inexpensive starting material without using any extraordinary production equipment such as a very-low-temperature reactor.Thus, this invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises permitting a lithium amide to act upon a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative at not below −20° C. Further, this invention also provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises treating a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative with a Grignard reagent to prepare a mixture of a compound and an acetic acid ester of the above formula (I), and permitting a lithium amide to act upon the mixture at a temperature not below −20° C. This invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid, a useful pharmaceutical intermediate, easily from a readily available, inexpensive starting material without using any extraordinary production equipment such as a very-low temperature reactor. Thus, this invention provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises permitting a lithium amide to act upon a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative at not below −20° C. Further, this invention also provides a process for producing a 5-hydroxy-3-oxopentanoic acid which comprises treating a mixture of an acetic acid ester and a 3-hydroxypropionic acid derivative with a Grignard reagent to prepare a mixture of a compound and an acetic acid ester of the above formula (I), and permitting a lithium amide to act upon the mixture at a temperature not below −20° C.

    Process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl] acetic acid derivatives
    10.
    发明授权
    Process for preparing optically active 2-[6-(hydroxy-methyl)-1,3-dioxan-4-yl] acetic acid derivatives 失效
    光学活性的2- [6-（羟基 - 甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法

    公开(公告)号：US07094594B2

    公开(公告)日：2006-08-22

    申请号：US10048553

    申请日：2001-06-05

    申请人： Akira Nishiyama ,  Miho Horikawa ,  Yoshihiko Yasohara ,  Noboru Ueyama ,  Kenji Inoue

    发明人： Akira Nishiyama ,  Miho Horikawa ,  Yoshihiko Yasohara ,  Noboru Ueyama ,  Kenji Inoue

    IPC分类号： C12P41/00

    CPC分类号： C07D319/06 ,  C12P7/42 ,  C12P17/06

    摘要： The present invention is to provide a production technology by which an optically active 2-[6-(hydroxymethyl)-1, 3-dioxan-4-yl]acetic acid derivative, which are of value as pharmaceutical intermediates, can be produced from inexpensive and readily available starting materials without using any extraordinary equipment such as an ultra-low-temperature reactor.The present invention is a production process of an optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivative which comprises reacting an enolate, prepared by permitting a base or a 0-valent metal to act on an acetic acid ester derivative with (S)-β-hydroxy-γ-butyrolactone at a temperature not lower than −30° C. to give a dihydroxyoxohexanoic acid derivative, treating the same with an acylating agent in the presence of a base to produce a dihydroxyoxohexanoic acid monoacyl derivative, reducing this compound with a microorganism to produce a trihydroxyhexanoic acid monoacyl derivative, treating this compound with an acetal-forming reagent in the presence of an acid catalyst to produce an acyloxymethyldioxanylacetic acid derivative, and finally, subjecting this compound to solvolysis in the presence of a base.

    摘要翻译： 本发明提供一种生产技术，通过该技术，可以从廉价的方式制备价值为药物中间体的光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物 和容易获得的起始材料，而不使用任何非常设备，例如超低温反应器。 本发明是光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的制备方法，该方法包括使通过使碱或0价金属 在不低于-30℃的温度下用（S）-β-羟基-γ-丁内酯在乙酸酯衍生物上作用，得到二羟基氧代己酸衍生物，在酰化剂存在下用酰化剂处理 碱化以制备二羟基氧己基单酰基衍生物，用微生物还原该化合物以产生三羟基己酸单酰基衍生物，在酸催化剂存在下用缩醛形成试剂处理该化合物，得到酰氧基甲基二恶烷基乙酸衍生物，最后， 该化合物在碱存在下溶剂解。