CAS: 37159-60-7; 3-Bromo-5-Chloro-1,2,4-Thiadiazole

该化合物是三环化合物,其特点是有硫氮原子环,由五人环结构中的两个氮原子和一个硫原子组成;该化合物的特点是三处的溴替代物和五处的氨基组,有助于其在各个领域(包括制药和农用化学)的活性和潜在应用;该物质一般是室温下的固体,在极地溶剂中可能表现出中等溶解性;溴原子的存在可增强其电子哲学特性,使其在核细胞替代反应中有用;此外,氨基化合物可参与氢结合,影响其与生物目标的相互作用;该化合物的独特结构允许进行多种化学改变,从而能够发展具有定制特性的衍生物.

结构式图片

欧盟法规

C&L通报

合成工艺路线路线简述

    📜二-(3-溴-1,2,4-噻二唑-5-基)-二硫醚置于氯体系中,用 溶剂黄146 用作溶剂,化学反应生成3-溴-5-氯-1,2,4-噻重氮
    参考文献:部分1,2,4-噻二唑基-亚磺酰氯的合成及性质
    标题:部分1,2,4-噻二唑基-亚磺酰氯的合成及性质
    摘要:由n-氰基-亚氨二硫代碳酸的二钾盐与氯气生成3-氯-1,2,4-噻二唑-5-亚磺酰氯,在潮湿空气中变为双-3-氯-1,2,4-噻二唑基-(5)--二硫化物(9)分解;1与溴反应形成双-3-溴-1,2,4-噻二唑基-(5)--二硫化物,后者与伯胺形成相应的次磺酰胺.
    Doi:10.1002/ardp.19723050511

    专利信息


    专利号:US-9481659-B2
    优先权日:2011-05-13
    标 题 :Selective heterocyclic sphingosine 1 phosphate receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM RICHARD
    权利人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM RICHARD; CELGENE INT II SÀRL
    摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

    专利号:US-9795613-B2
    优先权日:2014-12-10
    标题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK
    权利人:CELGENE INT II SÀRL
    摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

    专利号:US-9187522-B2
    优先权日:2011-12-12
    标题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
    权利人:RECEPTOS INC
    摘要:The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

    专利号:US-9598430-B2
    优先权日:2013-06-11
    标 题 :GLP-1 receptor modulators
    发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
    权利人:RECEPTOS INC; CELGENE INT II SÀRL
    摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

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    合成参考文献


    参考文献:10.1007/s12200-018-0855-4
    摘要:Guo R, Zhang W, Zhang Q, Lv X, Wang L. Efficient deep red phosphorescent OLEDs using 1,2,4-thiadiazole core-based novel bipolar host with low efficiency roll-off. Frontiers of Optoelectronics. 2018 Dec;11(4):375–84. doi: 10.1007/s12200-018-0855-4.
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