CAS: 145013-05-4; N,N'-Bis-Tert-Butoxycarbonylthiourea

该化合物是一种化学化合物,其独特结构包括两个与硫尿素(Thiourea modio)相连的三丁基碳酸(Boc)组,通常用于有机合成,特别是用于制作各种衍生物和药用化学中间体,具有有机溶剂溶解性等特性,适合各种反应.Boc保护组的存在允许在特定条件下有选择地取消保护,促进硫尿的进一步功能化.此外,硫尿因其生物活动而为人所知,其中可包括抗微生物和抗脉冲特性.该化合物的稳定性和再活性可能受到三丁基组提供的障碍的影响,使它成为合成化学中有价值的建筑块.与许多化学物质一样,处理应当谨慎进行,并遵循具有潜在毒性和再活性的适当安全议定书.

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合成工艺路线路线简述

    二碳酸二叔丁酯置于碳酸氢钠,硫脲体系中,用 四氢呋喃 用作溶剂,以60%的收率获得n,N'-二-Boc-硫脲
    参考文献:Derivatives Of Pyrimido[6.1-A]Isoquinolin-4-One
    标题:Derivatives Of Pyrimido[6.1-A]Isoquinolin-4-One
    摘要:该发明提供了通式(i)的化合物或其盐: 其中,R1和rx分别独立表示c1-6烷基或c2-7酰基;X表示och2或cr3R4基团;R3或r4分别独立表示氢原子或c1-3烷基;R5表示氢原子或c1-3烷基,C2-3烯基或c2-3炔基;R6表示氢原子或c1-6烷基,C2-6烯基,C2-6炔基,氨基,C1-6烷基氨基,二(c1-6)烷基氨基或c2-7酰氨基;R7和r8分别独立表示氢或卤素原子,羟基,三氟甲基,C1-6烷基,C2-6烯基,C2-6炔基,C2-7酰基,C1-6烷基硫基,C1-6烷氧基,C3-6环烷基;R9表示氢或卤素原子,羟基,三氟甲基,C1-6烷基,C2-6烯基,C2-6炔基,C2-7酰基,C1-6烷基硫基,C1-6烷氧基或c3-6环烷基.该化合物或其盐可用于治疗哮喘等呼吸系统疾病.该发明的化合物比已知的化合物特雷昆辛(9,10-二甲氧基-3-甲基-2-间二甲苯亚基-2,3,6,7-四氢-4H-嘧啶并[6,1-A]异喹啉-4-酮)具有更长的作用持续时间.

    海关参考信息

    专利信息


    专利号:WO-2008105759-A1
    优先权日:2007-02-27
    标 题:Methods for synthesis of modified peptides
    发明人:BROWER JUSTIN O
    权利人:ARGOLYN BIOSCIENCE INC; BROWER JUSTIN O
    摘要:Methods for the synthesis of peptides and peptide analogs containing aminoacid residues bearing substituted amino- and guanido- sidechains, such as alkyl lysine and arginine residues, are provided.

    专利号:US-7888337-B2
    优先权日:2007-08-31
    标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity
    发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG
    权利人:ACADEMIA SINICA
    摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.

    专利号:EP-1567195-B1
    优先权日:2002-11-26
    标题 :Dendrimer conjugates for selective solubilisation of protein aggregates
    发明人:HEEGAARD PETER; BOAS ULRIK
    权利人:UPFRONT CHROMATOGRAPHY AS
    摘要:Dendrimer conjugates are presented, which are formed between a dendrimer and a protein solubilising substance. Such dendrimer conjugates ar effective in the treatment of protein aggregate-related diseases (e.g. prion-related diseases). The protein solubilising substance and the dendrimer together show a protein aggregate solubilising effect higher than a physical mixture of the dendrimer and the protein solubilising substance (i.e. a synergistic effect). Such dendrimer conjugates are useful in the treatment or prevention of protein aggregate-relates diseases, in disinfection/decontamination processes and in classifying or identifying protein aggregates. The synthesis of such dendrimer conjugates from readily-available starting materials is described.

    专利号:US-2004053999-A1
    优先权日:1997-09-17
    标题 :Novel compounds and methods for synthesis and therapy
    发明人:BISCHOFBERGER NORBERT W; DAHL TERRENCE C; HITCHCOCK MICHAEL J M; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; MILLS ROGER G; WILLIAMS MATTHEW A
    摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

    专利号:US-6225341-B1
    优先权日:1995-02-27
    标 题:Compounds and methods for synthesis and therapy
    发明人:BISCHOFBERGER NORBERT W; KIM CHOUNG U; LEW WILLARD; LIU HONGTAO; WILLIAMS MATTHEW A
    权利人:GILEAD SCIENCES INC
    摘要:Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods of inhibiting neuraminidase in samples suspected of containing neuraminidase are also described. Antigenic materials, polymers, antibodies, conjugates of the compounds of the invention with labels, and assay methods for detecting neuraminidase activity are also described.

    专利号:WO-0009116-A1
    优先权日:1998-08-14
    标 题:Grp receptor ligands
    发明人:XIANG JIA-NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV
    权利人:SMITHKLINE BEECHAM CORP; XIANG JIA NING; KARPINSKI JOSEPH M; CHRISTENSEN SIEGFRIED B IV
    摘要:Novel GRP receptor antagonists are provided. Methods of using the present compounds to antagonize GRP receptors are also provided. The present invention further involves the synthesis of the present compounds.
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    合成参考文献


    摘要:Huy, P.; Czekelius, C., Science of Synthesis Knowledge Updates, (2019) 2, 143.
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