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1.发明授权2'-fluorofuranosyl derivatives and novel method of preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides 失效2'-氟代呋喃糖苷衍生物和制备2'-氟嘧啶和2'-氟嘌呤核苷的新方法
公开(公告)号：US5336764A
公开(公告)日：1994-08-09
申请号：US968567
申请日：1992-10-29
IPC分类号： C07H1/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/18 , C07H13/08 , C07H15/04 , C07H15/203 , C07H19/06 , C07H19/10 , C07H19/16 , C07H23/00 , C07G3/00
摘要： A compound has the formula ##STR1## wherein R is selected from the group consisting of (C.sub.7 -C.sub.20)aroyl, (C.sub.6 -C.sub.20)aryl, aralkyl and alkylaryl, and (C.sub.1 -C.sub.10)alkyl-di(C.sub.6 -C.sub.20)aryl Si, R' is selected from the group consisting of (C.sub.1 -C.sub.10)alkyl, (C.sub.7 -C.sub.20)aroyl and (C.sub.2 -C.sub.12)acyl, all of which may be further substituted with O, S, N or alkyl, and R'" is selected from the group consisting of halogen, (C.sub.1 -C.sub.10)alkoxy, (C.sub.1 -C.sub.10)acyloxy, O-methane-sulfonyl and O-p-toluenesulfonyl. A composition of matter comprises 0.001 to 99.999 wt % of the above compound.
摘要翻译： 化合物具有下式（IMAGE），其中R选自（C 7 -C 20）芳酰基，（C 6 -C 20）芳基，芳烷基和烷芳基，和（C 1 -C 10）烷基 - 二（C 6 -C 20）芳基 Si，R'选自（C 1 -C 10）烷基，（C 7 -C 20）芳酰基和（C 2 -C 12）酰基，所有这些可以进一步被O，S，N或烷基取代，R “选自卤素，（C 1 -C 10）烷氧基，（C 1 -C 10）酰氧基，O-甲磺酰基和对甲苯磺酰基。 物质组合物含有0.001〜99.999重量％的上述化合物。
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2.发明申请公开(公告)号：US20110111959A1
公开(公告)日：2011-05-12
申请号：US12732938
申请日：2010-03-26
IPC分类号： A01N43/72 , C07D215/36 , C07D217/22 , C07D279/12 , C07D223/14 , A01N43/46 , A01N43/60 , A01N43/40 , A01P21/00
CPC分类号： C07D215/58 , A01N43/42 , C07D217/22 , A01N25/00
摘要： This disclosure relates, inter alia, to stimulants of pollen tube germination and growth of pollen tubes, and methods of their use to stimulate in vitro and in vivo pollen germination and pollen tube growth.
摘要翻译： 本公开尤其涉及花粉管萌发和花粉管生长的兴奋剂，以及它们用于刺激体外和体内花粉萌发和花粉管生长的方法。
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公开(公告)号：US08389728B2
公开(公告)日：2013-03-05
申请号：US12732938
申请日：2010-03-26
IPC分类号： C07D215/38
CPC分类号： C07D215/58 , A01N43/42 , C07D217/22 , A01N25/00
摘要： This disclosure relates, inter alia, to stimulants of pollen tube germination and growth of pollen tubes, and methods of their use to stimulate in vitro and in vivo pollen germination and pollen tube growth.
摘要翻译： 本公开尤其涉及花粉管萌发和花粉管生长的兴奋剂，以及它们用于刺激体外和体内花粉萌发和花粉管生长的方法。
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4.发明授权2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides 失效2'-氟呋喃糖苷衍生物及其制备方法2'-氟嘧啶核苷和2'-氟嘌呤核苷
公开(公告)号：US5817799A
公开(公告)日：1998-10-06
申请号：US556713
申请日：1990-07-23
IPC分类号： C07H1/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61K31/7076 , A61P31/12 , A61P31/18 , C07H13/08 , C07H15/04 , C07H15/203 , C07H19/06 , C07H19/10 , C07H19/16 , C07H23/00
摘要： A method of preparing a 2'-fluoro compound of the formula ##STR1## where B is selected from the group consisting of purines and pyrimidines, both of which may be substituted, comprises reacting a compound of the formula II(a) or II(b) ##STR2## where R and R' are as defined in the specification with an acid halide under conditions effective to obtain a halide of the formula ##STR3## where X is a halogen. A silane of the formula B-Si (R").sub.3 where R" is as defined in the specification, is added to this product (III) under conditions effective to obtain a compound of the formula (IV) ##STR4## The compound of formula (IV) is reacted with a reagent selected from the group consisting of ammonia, BCl.sub.3 and ((C.sub.1 -C.sub.10)alkyl).sub.4 NF, under conditions effective to obtain the compound of formula (I). The compounds of formula (I) resulting from these methods exhibit anti-HIV activities and are useful for therapy against the HIV virus.
摘要翻译： 制备式（I）的2'-氟化合物的方法，其中B选自嘌呤和嘧啶，它们都可以被取代，包括使式II（a）的化合物与式 （IIa）（IIb）其中R和R'如本说明书中所定义，与有效得到式（III）的卤化物的条件下的酰卤相同，其中X 是卤素。 在有效获得式（IV）化合物的条件下，将式B-Si（R“）3的硅烷（其中R”如说明书中所定义）加入到该产物（III）中 IV）在有效获得式（I）化合物的条件下，使式（IV）化合物与选自氨，BCl 3和（（C 1 -C 10）烷基）4 NF的试剂反应。 由这些方法得到的式（I）化合物表现出抗HIV活性，可用于治疗HIV病毒。
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