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公开(公告)号：US06750064B2
公开(公告)日：2004-06-15
申请号：US09752857
申请日：2000-12-28
IPC分类号： G01N122
CPC分类号： G01N25/147 , B01J2219/00522 , B01J2219/00585 , B01J2219/00599 , B01J2219/00702 , B01J2219/00725 , B01J2219/00756 , B01L3/06 , C30B7/00 , C40B40/10 , C40B50/08 , Y10T436/25 , Y10T436/2575 , Y10T436/25875
摘要： Methods for searching for possible forms of a sample and methods of screening a sample according to its form comprise disposing the sample in at least one receptacle that defines a capillary space, such as a capillary tube. The sample is solidified to generate at least one solid form or semisolid form, and the generated form is analyzed and classified. The analysis may determine differences in molecular arrangement of the various forms or characteristics that reflect the form. The methods may employ a plurality of samples, conditions, or receptacles in an effort to generate a variety of forms, so that all or a high percentage of possible forms are obtained.
摘要翻译： 用于搜索样品的可能形式的方法和根据其形式筛选样品的方法包括将样品设置在限定毛细管空间的至少一个容器中，例如毛细管。 将样品固化以产生至少一种固体形式或半固体形式，并且对所生成的形式进行分析和分类。 分析可以确定反映形式的各种形式或特征的分子排列的差异。 这些方法可以采用多个样本，条件或容器来努力产生各种形式，使得获得全部或高百分比的可能形式。
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公开(公告)号：US4710581A
公开(公告)日：1987-12-01
申请号：US783419
申请日：1985-10-03
IPC分类号： C07C205/56 , C07C79/46
CPC分类号： C07C201/12 , C07C201/16
摘要： Halonitroarylacetic acid esters are prepared by reacting a halonitroaromatic compound with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base. The halonitroarylacetic acid esters formed by the process can be readily converted into derivatives, such as pharmaceuticals.
摘要翻译： 卤代四芳基乙酸酯通过卤代硝基芳族化合物与α，α-二取代的乙酸酯在惰性溶剂中和在碱的存在下反应来制备。 通过该方法形成的卤代硝酰基乙酸酯可以容易地转化为衍生物，例如药物。
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公开(公告)号：US4502995A
公开(公告)日：1985-03-05
申请号：US452518
申请日：1982-12-23
IPC分类号： C07C63/33 , C07C255/32 , C07C121/50
CPC分类号： C07C255/00
摘要： Fluoronitrolarylacetonitriles are prepared by reacting a fluoronitroaromatic compound having a nitro substituent, at least one fluoro substituent, and at least one replaceable hydrogen on (1) a benzene ring bearing at least one other innocuous substituent, (2) a heterocyclic aromatic ring, or (3) a carbocyclic aromatic ring of a polycyclic ring structure with an alpha,alpha-disubstituted acetonitrile in an inert solvent and in the presence of a base so that the nitrile undergoes a nucleophilic substitution on an unsubstituted ring carbon of the fluoronitroaromatic compound during which an alpha-substituent functions as a leaving group.
摘要翻译： 氟化芳基芳基乙腈通过在（1）含有至少一个其他无害取代基的苯环上反应具有硝基取代基的氟代芳基化合物，至少一个氟取代基和至少一个可取代的氢，（2）杂环芳族环或（ 3）具有α，α-二取代的乙腈的多环环结构的碳环芳环在惰性溶剂中并在碱的存在下，使得腈在氟代芳族化合物的未取代的环碳上经历亲核取代，其中 α-取代基用作离去基团。
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公开(公告)号：US4476315A
公开(公告)日：1984-10-09
申请号：US452616
申请日：1982-12-23
IPC分类号： C07C205/56 , C07C79/46
CPC分类号： C07C201/12 , C07C201/16 , C07C227/04 , C07C253/30 , C07C67/317
摘要： Nitroarylacetic acid esters are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base so that the ester undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their esters are useful intermediates for the synthesis of pharmaceuticals.
摘要翻译： 硝基芳基乙酸酯通过在惰性溶剂中和在碱的存在下使含有硝基的芳环上的无卤素的硝基芳族化合物与α，α-二取代的乙酸酯反应来制备，使得酯经历 在其中α取代基用作离去基团的硝基芳族化合物的未取代环碳上的亲核取代。 硝基苯乙酸及其酯是合成药物的有用中间体。
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公开(公告)号：US4511729A
公开(公告)日：1985-04-16
申请号：US474137
申请日：1983-03-10
IPC分类号： C07C205/56 , C07C79/46
CPC分类号： C07C201/12 , C07C227/04 , C07C67/317
摘要： Nitrophenoxy- or nitrophenylthiobenzeneacetic acid esters are prepared by reacting a nitrophenoxy- or nitrophenylthiobenzene with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base. The products are useful as intermediates for the synthesis of pharmaceuticals, such as fenoprofen.
摘要翻译： 硝基苯氧基 - 或硝基苯基硫代苯乙酸酯通过硝基苯氧基 - 或硝基苯基硫代苯与α，α-二取代的乙酸酯在惰性溶剂中并在碱的存在下反应来制备。 该产品可用作合成药物的中间体，例如非诺洛芬。
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6.发明授权
公开(公告)号：US4581463A
公开(公告)日：1986-04-08
申请号：US640004
申请日：1984-08-10
IPC分类号： C07C205/56 , C07D209/46 , C07C79/46 , C07D207/18
CPC分类号： C07C201/12 , C07C201/16 , C07C227/04 , C07C67/343
摘要： Halonitroarylacetic acid esters are prepared by reacting a halonitroaromatic compound with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base. The halonitroarylacetic acid esters formed by the process can be readily converted into derivatives, such as pharmaceuticals.
摘要翻译： 卤代四芳基乙酸酯通过卤代硝基芳族化合物与α，α-二取代的乙酸酯在惰性溶剂中和在碱的存在下反应来制备。 通过该方法形成的卤代硝酰基乙酸酯可以容易地转化为衍生物，例如药物。
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公开(公告)号：US4502998A
公开(公告)日：1985-03-05
申请号：US474138
申请日：1983-03-10
IPC分类号： C07C255/32 , C07C121/50
CPC分类号： C07C255/00
摘要： Nitrophenoxy- or phenylthiobenzeneacetonitriles are prepared by reacting a nitrophenoxy- or nitrophenylthiobenzene with an alpha,alpha-dinitrosubstituted acetonitrile in an inert solvent and in the presence of a base. The products are useful as intermediates for the synthesis of pharmaceuticals, such as fenoprofen.
摘要翻译： 硝基苯氧基或苯硫基苯乙腈通过硝基苯氧基或硝基苯基硫代苯与α，α-二硝基取代的乙腈在惰性溶剂中和在碱的存在下反应来制备。 该产品可用作合成药物的中间体，例如非诺洛芬。
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公开(公告)号：US4499026A
公开(公告)日：1985-02-12
申请号：US452618
申请日：1982-12-23
IPC分类号： C07C255/32 , C07C121/50
CPC分类号： C07C255/00
摘要： Nitroarylacetonitriles are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetonitrile in an inert solvent and in the presence of a base so that the nitrile undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their nitriles are useful intermediates for the synthesis of pharmaceuticals.
摘要翻译： 硝基芳基乙腈通过在惰性溶剂中和在碱的存在下使含有硝基的芳族环上没有卤素的硝基芳族化合物与α，α-二取代的乙腈反应来制备，使得腈在 其中α-取代基用作离去基团的硝基芳族化合物的未取代的环碳。 硝基苯乙酸及其腈是合成药物的有用中间体。
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公开(公告)号：US07041169B2
公开(公告)日：2006-05-09
申请号：US10688123
申请日：2003-10-17
IPC分类号： C30B7/14
CPC分类号： C30B7/00 , C30B29/54 , G01N1/40 , G01N1/44 , G01N2001/4027 , Y10T436/25 , Y10T436/25375 , Y10T436/25875
摘要： A method for generating and isolating a high free energy form of a compound or a mixture of compounds comprises the steps of placing a sample in a capillary tube, solidifying the sample in the capillary tube, and isolating a high free energy form of the sample. A method for searching for a high free energy form of a sample comprises the steps of placing the compound or mixture in a capillary tube, generating a solid in the capillary tube, and determining whether a high free energy form of the sample was generated. The sample may be a compound or mixture.
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10.发明授权Methods of generating and screening for high free energy forms in capillaries 有权在毛细血管中产生和筛选高自由能形式的方法公开(公告)号：US06642060B2
公开(公告)日：2003-11-04
申请号：US09752788
申请日：2000-12-28
IPC分类号： G01N100
CPC分类号： C30B7/00 , C30B29/54 , G01N1/40 , G01N1/44 , G01N2001/4027 , Y10T436/25 , Y10T436/25375 , Y10T436/25875
摘要： A method for generating and isolating a high free energy form of a compound or a mixture of compounds comprises the steps of placing a sample in a capillary tube, solidifying the sample in the capillary tube, and isolating a high free energy form of the sample. A method for searching for a high free energy form of a sample comprises the steps of placing the compound or mixture in a capillary tube, generating a solid in the capillary tube, and determining whether a high free energy form of the sample was generated. The sample may be a compound or mixture.
摘要翻译： 用于产生和分离化合物或化合物混合物的高自由能形式的方法包括以下步骤：将样品置于毛细管中，固定毛细管中的样品，以及分离样品的高自由能形式。 用于搜索样品的高自由能形式的方法包括以下步骤：将化合物或混合物置于毛细管中，在毛细管中产生固体，并确定是否产生高自由能形式的样品。 样品可以是化合物或混合物。
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