Method of making PNA oligomers
    2.
    发明申请
    Method of making PNA oligomers 有权
    制备PNA低聚物的方法

    公开(公告)号:US20060003374A1

    公开(公告)日:2006-01-05

    申请号:US11182936

    申请日:2005-07-15

    摘要: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

    摘要翻译: 本申请涉及用于制备PNA(肽核酸)寡聚体的通式(I)的单体,并提供合成预定义的序列PNA寡聚体和随机序列PNA寡聚体的方法:其中E为氮或C-R' ; J为硫或氧; R',R 1,R 2,R 3,R 4独立地是H,卤素,烷基,硝基,腈,烷氧基,卤代烷基,卤代烷氧基,苯基或卤代苯基,R 5是H或被保护或未被保护的天然或非天然α- 氨基酸; 并且B是天然或非天然核碱基,其中当所述核碱基具有环外氨基功能时,所述功能受到在硫醇存在下对酸不稳定但对弱至中碱稳定的保护基保护。

    PNA monomer and precursor
    6.
    发明申请
    PNA monomer and precursor 有权
    PNA单体和前体

    公开(公告)号:US20050250786A1

    公开(公告)日:2005-11-10

    申请号:US11183025

    申请日:2005-07-15

    摘要: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrite, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

    摘要翻译: 本申请涉及用于制备PNA(肽核酸)寡聚体的通式(I)的单体,并提供合成预定义的序列PNA寡聚体和随机序列PNA寡聚体的方法:其中E为氮或C-R' ; J为硫或氧; R',R 1,R 2,R 3,R 4独立地为H,卤素,烷基,硝基,亚硝酸根,烷氧基,卤代烷基,卤代烷氧基,苯基或卤代苯基,R 5为H或保护或未保护的天然或非天然α- 氨基酸; 并且B是天然或非天然核碱基,其中当所述核碱基具有环外氨基功能时,所述功能受到在硫醇存在下对酸不稳定但对弱至中碱稳定的保护基保护。

    PNA monomer and precursor
    7.
    发明申请
    PNA monomer and precursor 有权
    PNA单体和前体

    公开(公告)号:US20050026930A1

    公开(公告)日:2005-02-03

    申请号:US10819769

    申请日:2004-04-06

    摘要: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is sulfur or oxygen; J is nitrogen or C—R′; R1, R′ is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy or a functional group having one of following general formulae: wherein A1, A2, A3, A4, A5, is independently selected from H, halogen such as F, Cl, Br or I, CF3, alkyl, preferably C1-C4 alkyl, nitro, nitrile, alkoxy, preferably C1-C4 alkoxy, halogenated (such as F, Cl, Br and I) alkyl, preferably halogenated C1-C4 alkyl, halogenated (such as F, Cl, Br and I) alkoxy, preferably halogenated C1-C4 alkoxy, phenyl, and halogenated (such as F, Cl, Br and I phenyl; R2 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

    摘要翻译: 本申请涉及用于制备PNA(肽核酸)寡聚体的通式(I)的单体,并提供合成预定义的序列PNA寡聚体和随机序列PNA寡聚体的方法:其中E为硫或氧; J为氮或C-R'; R1,R'独立地为H,卤素,烷基,硝基,腈,烷氧基,卤代烷基,卤代烷氧基或具有以下通式之一的官能团:其中A1,A2,A3,A4,A5独立地选自H ,卤素如F,Cl,Br或I,CF 3,烷基,优选C 1 -C 4烷基,硝基,腈,烷氧基,优选C 1 -C 4烷氧基,卤代(如F,Cl,Br和I)烷基, C 1 -C 4烷基,卤代(如F,Cl,Br和I)烷氧基,优选卤代C 1 -C 4烷氧基,苯基和卤代(如F,Cl,Br和I苯基; R2是H或被保护或未被保护的一侧 天然或非天然α-氨基酸的链; B是天然或非天然核碱基,其中当所述核碱基具有外来氨基功能时,所述功能受到对酸不稳定的保护基保护,但在弱碱性至中等碱基中稳定 存在硫醇。

    Process for the Preparation of 11-(4-[2-(2-Hydroxyethoxy)Ethyl]-I-Piperazinyl)Dibenzo[b,f][I,4]Thiazepine
    9.
    发明申请
    Process for the Preparation of 11-(4-[2-(2-Hydroxyethoxy)Ethyl]-I-Piperazinyl)Dibenzo[b,f][I,4]Thiazepine 失效
    制备11-(4- [2-(2-羟基乙氧基)乙基] -1-哌嗪基)二苯并[b,f] [I,4]噻吩

    公开(公告)号:US20070225494A1

    公开(公告)日:2007-09-27

    申请号:US11571116

    申请日:2005-06-17

    IPC分类号: C07D281/12

    CPC分类号: C07D281/16

    摘要: Disclosed is a process for the preparation of 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine. In the process, low-priced 2,2′-dithiosalicylic acid as starting material is subjected to bond formation reaction with 1-chloro-2-nitrobenzene in a basic aqueous solution, a nitro group reduction reaction is conducted, cyclization and chlorination reactions are simultaneously carried out in the presence of a equivalent amount of halogenating agent, a reaction with piperazine is continuously conducted without separation, and a reaction with 2-haloethoxyethanol is conducted, thereby it is possible to economically producing Quetiapine, that is, 11-(4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl)-dibenzo[b,f][1,4]thiazepine, in an environmentally friendly manner. Particularly, the process is advantageous in that economic efficiency is assured because of use of the low-priced starting material, use of an organic solvent is minimized because a reaction is conducted in an aqueous solution, and it is possible to achieve the environmentally friendly and economical process having high commercial usefulness because the number of reaction steps of the process is reduced and because generation of acidic waste is minimized.

    摘要翻译: 公开了制备11-(4- [2-(2-羟基乙氧基)乙基] -1-哌嗪基) - 二苯并[b,f] [1,4]硫杂吖庚因的方法。 在此过程中,作为起始原料的低价2,2'-二硫代水杨酸与碱性水溶液中的1-氯-2-硝基苯进行结合形成反应,进行硝基还原反应,环化反应和氯化反应 在等量的卤化剂的存在下同时进行,与哌嗪的反应在不分离的情况下连续进行,与2-卤代乙氧基乙醇进行反应,从而可以经济地制备喹硫平,即11-(4 - [2-(2-羟基乙氧基)乙基] -1-哌嗪基) - 二苯并[b,f] [1,4]硫杂吖庚因。 特别地,该方法的优点在于,由于使用低价起始材料来确保经济效率,因此在水溶液中进行反应而使有机溶剂的使用最小化,并且可以实现环境友好和 经济的方法具有很高的商业用途,因为该方法的反应步骤的数量减少并且由于酸性废物的产生被最小化。

    Communication terminal
    10.
    发明申请
    Communication terminal 有权
    通讯终端

    公开(公告)号:US20070103457A1

    公开(公告)日:2007-05-10

    申请号:US11546352

    申请日:2006-10-12

    申请人: Sang Ahn Jong Lim

    发明人: Sang Ahn Jong Lim

    IPC分类号: G09G5/00

    摘要: A communication terminal equipped with a sliding-type flat display module includes a main body and a flat display which slides between retracted and extended positions along a first axis relative to the main body and which rotates to a tilted position along a second axis when in the extended position. The first axis may be substantially perpendicular to the second axis. In the retracted position, the flat display is unable to rotate to the tilted position along the second axis. Also, in this position, the display is partially visible to allow information to be read by a user while at the same time being protected within a receiving part of the terminal.

    摘要翻译: 具有滑动型平板显示模块的通信终端包括主体和平面显示器,其在相对于主体的第一轴线的缩回位置和延伸位置之间滑动,并且当在第二轴线处于第二轴线时旋转到倾斜位置 延长位置 第一轴线可以基本上垂直于第二轴线。 在缩回位置,平面显示器不能沿着第二轴线旋转到倾斜位置。 此外,在该位置,显示器是部分可见的,以允许用户读取信息,同时在终端的接收部分内受到保护。