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    Process for the preparation of 9-deazaguanine derivatives
    3.
    发明授权
    Process for the preparation of 9-deazaguanine derivatives 失效
    9-脱氮鸟嘌呤衍生物的制备方法

    公开(公告)号：US06946554B2

    公开(公告)日：2005-09-20

    申请号：US10878035

    申请日：2004-06-29

    申请人： Arthur J. Elliott ,  David A. Walsh ,  Philip E. Morris

    发明人： Arthur J. Elliott ,  David A. Walsh ,  Philip E. Morris

    IPC分类号： A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  C07D487/04 ,  C07D207/34

    CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541

    摘要： Derivatives of 9-deazaguanine of the formula I: are prepared by reacting an aldehyde or ketone of the formula II: with a dialkylaminomalonate to produce an enamine. The enamine is then reacted with a base to produce a pyrrole represented by the formula: The pyrrole is reacted with a compound represented by the formula R3OC(O)N═C(Z)NHC(O)OR3 or a derivative of carbamimidoic acid to provide a protected guanidine compound. The guanidine compound is converted to the desired deazaguanine by reaction with 1) trifluoracetic acid or 2) C1-C4 alkoxide or alkali metal or alkaline earth metal hydroxide followed by neutralization with an acid.

    摘要翻译： 式I的9-脱氮鸟嘌呤的衍生物通过使式II的醛或酮与二烷基氨基马来酸盐反应以制备烯胺来制备。 然后将烯胺与碱反应以产生由下式表示的吡咯：吡咯与由式R 3 OC（O）NC（Z）NHC（O）OR表示的化合物反应 3或氨基甲脒酸的衍生物，以提供受保护的胍化合物。 胍化合物通过与1）三氟乙酸或2）C 1 -C 4烷醇盐或碱金属或碱土金属氢氧化物反应而转化为所需的脱氮鸟嘌呤，随后中和 与酸。

    Process for the preparation of 9-deazaguanine derivatives
    4.
    发明授权
    Process for the preparation of 9-deazaguanine derivatives 失效
    9-脱氮鸟嘌呤衍生物的制备方法

    公开(公告)号：US5650511A

    公开(公告)日：1997-07-22

    申请号：US570786

    申请日：1995-12-12

    申请人： Arthur J. Elliott ,  David A. Walsh

    发明人： Arthur J. Elliott ,  David A. Walsh

    IPC分类号： C07D487/04 ,  C07C255/27 ,  C07F9/6506

    CPC分类号： C07D487/04

    摘要： Derivatives of 9-deazaguanine are prepared by reacting an aldehyde or ketone with a dialkylaminomalonate to form the corresponding enamine. The enamine is then reacted with a base to form a cyclic pyrrole. The cyclic pyrrole is reacted with an urea compound to provide a protected guanidino compound. The guanidino is converted to the desired 9-deazaguanine derivative by reacting with trifluoracetic acid or with an alkoxide or hydroxide followed by neutralization with an acid.

    摘要翻译： 9-取代鸟嘌呤的衍生物通过使醛或酮与二烷基氨基马来酸盐反应形成相应的烯胺制备。 然后将烯胺与碱反应形成环状吡咯。 使环状吡咯与脲化合物反应，得到保护的胍基化合物。 胍基通过与三氟乙酸或与醇盐或氢氧化物反应，随后与酸中和而转化为所需的9-脱氮鸟嘌呤衍生物。

    1-Aryl-1-(1H-azol-1-ylalkyl)-1,3-dihydroisobenzofurans, related derivatives and pharmaceutical compositions thereof useful as antifungals
    7.
    发明授权
    1-Aryl-1-(1H-azol-1-ylalkyl)-1,3-dihydroisobenzofurans, related derivatives and pharmaceutical compositions thereof useful as antifungals 失效
    1-芳基-1-（1H-吡唑-1-基烷基）-1,3-二氢异苯并呋喃，可用作抗真菌剂的相关衍生物及其药物组合物

    公开(公告)号：US4877801A

    公开(公告)日：1989-10-31

    申请号：US183267

    申请日：1988-04-06

    申请人： Raymond G. Lovey ,  Arthur J. Elliott

    发明人： Raymond G. Lovey ,  Arthur J. Elliott

    IPC分类号： C07D405/06 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06

    摘要： Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiophenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.

    摘要翻译： 包括1-芳基-1-（1H-咪唑-1-基甲基）-1,3-二氢异苯并呋喃如1-（4-氯苯基）-1-（1H-咪唑-1-基甲基）-1,3- 二氢异苯并呋喃和1-芳基-1-（1H-1,2,4-三唑-1-基甲基）-1,3-二氢异苯并呋喃。 还公开了相应的苯并[c]噻吩，异苯并二氢吡喃和异噻菌灵和含有它们的抗真菌药物组合物，以及使用所述药物组合物在具有易感性抗真菌感染的温血动物中引发抗真菌反应的方法。

    Preparation of trifluoroethylamine
    8.
    发明授权
    Preparation of trifluoroethylamine 失效
    三氟乙胺的制备

    公开(公告)号：US4618718A

    公开(公告)日：1986-10-21

    申请号：US745058

    申请日：1985-06-14

    申请人： Arthur J. Elliott ,  Gary W. Astrologes

    发明人： Arthur J. Elliott ,  Gary W. Astrologes

    IPC分类号： C07C85/04

    CPC分类号： C07C209/08

    摘要： In the reaction of a 2,2,2-trifluoroethyl halide with ammonia to produce 2,2,2-trifluoroethylamine, the improvement which comprises effecting the reaction with from about 1 to 3 moles of ammonia per mole of the trifluoroethyl halide at a temperature of about 170.degree. to 240.degree. C. and a pressure less than about 300 psig in the presence of a substantially anhydrous inert solvent present in at least about the same molar amount as the trifluoroethyl halide. Advantageously the temperature is from about 200.degree. to 220.degree. C., the pressure is at most about 250 psig, the solvent is N-methylpyrrolidone present in at least about 3 times the molar amount of the trifluoroethyl halide, and the halide is the chloride.

    摘要翻译： 在2,2,2-三氟乙基卤化物与氨反应产生2,2,2-三氟乙胺的反应中，其改进包括在约1至3摩尔氨/摩尔三氟乙基卤化物的温度下进行反应 约170℃至240℃，压力小于约300psig，在基本无水的惰性溶剂存在下，以与三氟乙基卤化物至少约相同的摩尔量存在。 有利地，温度为约200至220℃，压力至多约250psig，溶剂为存在于三氟乙基卤化物摩尔量的至少约3倍的N-甲基吡咯烷酮，卤化物为氯化物 。

    1-aryl-1-(1H-azol-1-ylalkyl)-1,3-dihydroisobenzofurans, related derivatives and pharmaceutical compositions thereof useful as antifungals
    9.
    发明授权
    1-aryl-1-(1H-azol-1-ylalkyl)-1,3-dihydroisobenzofurans, related derivatives and pharmaceutical compositions thereof useful as antifungals 失效
    1-芳基-1-（1H-吡唑-1-基烷基）-1,3-二氢异苯并呋喃，可用作抗真菌剂的相关衍生物及其药物组合物

    公开(公告)号：US4737508A

    公开(公告)日：1988-04-12

    申请号：US697539

    申请日：1985-02-01

    申请人： Raymond G. Lovey ,  Arthur J. Elliott

    发明人： Raymond G. Lovey ,  Arthur J. Elliott

    IPC分类号： C07D405/06

    CPC分类号： C07D405/06

    摘要： Novel compounds including 1-aryl-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofurans such as 1-(4-chlorophenyl)-1-(1H-imidazol-1-ylmethyl)-1,3-dihydroisobenzofuran, and 1-aryl-1-(1H-1,2,4-trizazol-1-ylmethyl)-1,3-dihydroisobenzofurans are disclosed. The corresponding benzo[c]thiopenes, isochromans, and isothiochromans and antifungal pharmaceutical compositions containing same, and methods of using said pharmaceutical compositions to elicit an antifungal response in warm blooded animals having a susceptible antifungal infection are also disclosed.

    摘要翻译： 包括1-芳基-1-（1H-咪唑-1-基甲基）-1,3-二氢异苯并呋喃如1-（4-氯苯基）-1-（1H-咪唑-1-基甲基）-1,3- （1H-1,2,4-三唑-1-基甲基）-1,3-二氢异苯并呋喃和1-芳基-1-（1H-1,2,4-三唑-1-基甲基）-1,3-二氢异苯并呋喃。 还公开了相应的苯并[c]噻吩，异苯并二氢吡喃和异硫氰酸酯和含有它们的抗真菌药物组合物，以及使用所述药物组合物在具有易感性抗真菌感染的温血动物中引发抗真菌反应的方法。

    Coupling of chloroperfluoroalkanes
    10.
    发明授权
    Coupling of chloroperfluoroalkanes 失效
    氯全氟烷烃的偶联

    公开(公告)号：US4634797A

    公开(公告)日：1987-01-06

    申请号：US698989

    申请日：1985-02-07

    申请人： Arthur J. Elliott

    发明人： Arthur J. Elliott

    IPC分类号： C07C17/269 ,  B01J23/00 ,  C07B61/00 ,  C07C17/00 ,  C07C17/26 ,  C07C19/08 ,  C07C19/10 ,  C07C67/00

    CPC分类号： C07C17/269

    摘要： A process for the coupling of a chloroperfluoroalkane having a --CFCl.sub.2 moiety which comprises heating the alkane at a temperature of about 150.degree. to 260.degree. C. in the presence of at least about 0.1 times the molar amount each of copper and zinc at a mole ratio of copper:zinc from about 2:1 to 1:2. The product is obtained in relatively high yield and conversion.

    摘要翻译： 一种具有-CF 2 Cl 2部分的氯全氟烷烃的偶联方法，该方法包括在至少约0.1倍摩尔量的铜和锌的摩尔量存在下，在约150-260℃的温度下加热烷烃 铜：锌的比例为约2：1至1：2。 该产品以相对高的产率和转化率获得。