CAS: 13745-17-0; 4-Bromo-1H-Pyrazole-3-Carboxylic Acid

该化合物是制药和农用化学研究中广泛使用的一种多用途的杂交环状结构,其溴替代成分可增强交叉反应的回旋性,而碳球酸组则允许进一步发挥作用,使其在合成复杂分子时具有价值. 丙烯酸核心有助于其稳定性和生物活性,经常作为药物发现的关键中间体.该化合物对于发展动脉抑制剂和其他生物活性剂特别有用.其高纯度和定义明确的结构确保合成应用的一贯性.建议在惰性条件下进行适当的处理和储存以保持其完整性.

结构式图片

相似化合物

5932-34-3 81190-89-8 288246-16-2

欧盟法规

ECHA物质C&L通报

上下游产品

吡唑-3-甲酸 1H-Pyrazole-3-Carboxylic Acid 1621-91-6

合成工艺路线路线简述

    4-溴-1-苯基磺酰基吡唑-5-羧酸置于氢氧化钾体系中,用 甲醇 用作溶剂,化学反应 1.0H,以60%的收率获得4-溴-1H-吡唑-3-甲酸
    参考文献:Heinisch,Gottfried; Holzer,Wolfgang; Pock,Sabine,Journal Of The Chemical Society. Perkin Transactions I,1990,# 7,P. 1829-1834
    标题:Heinisch,Gottfried; Holzer,Wolfgang; Pock,Sabine,Journal Of The Chemical Society. Perkin Transactions I,1990,# 7,P. 1829-1834

    海关参考信息

    专利信息


    专利号:EP-2607355-A1
    优先权日:2011-12-23
    标 题:Synthesis of triazolopyrimidine compounds
    权利人:LEK PHARMACEUTICALS
    摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.

    专利号:EP-2666771-A1
    优先权日:2012-05-24
    标题 :Synthesis of Aminocyclopentanetriol Derivatives
    发明人:STERK DAMJAN; CASAR ZDENKO
    权利人:LEK PHARMACEUTICALS
    摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor. nThe present invention provides in particular a process for the preparation of a compound of formula Vn ncomprising: na) providing a compound of formula IVn n, and nb) reducing the compound of formula IV with activated zinc in the presence of copper to give the compound of formula V.

    专利号:US-9278972-B2
    优先权日:2011-12-23
    标题 :Synthesis of triazolopyrimidine compounds
    发明人:MARAS NENAD; GAZIC SMILOVIC IVANA; STERK DAMJAN
    权利人:LEK PHARMACEUTICALS
    摘要:The present invention relates to the field of organic synthesis and describes the synthesis of specific intermediates suitable for the preparation of triazolopyrimidine compounds such as ticagrelor.

    专利号:US-7001625-B2
    优先权日:2001-07-30
    标 题:Solid phase synthesis of salts of organic acids including butyric acid
    发明人:VAN DYCK STEFAAN; ADAMS CLIFFORD; MEEUSEN ANDRE; VAN CAMPENHOUT LEEN
    权利人:KEMIN IND INC
    摘要:A process for the solid-phase synthesis of salts of organic acids in a granular, free-flowing, and dust-free form particularly suited for use as animal feed additives. A mixture of liquid organic acids, including butyric acid, is applied to an inert, absorbent carrier. A solid base is then added during stirring. The acid is slowly released from the carrier preventing the fast reactions that lead to the formation of clumps. The exothermic reaction releases heat which assists in reducing the moisture content of the product. The addition of butyric acid results in a product which has an improved effect on animal growth over the animal feed additive without the addition of butyric acid.

    专利号:US-6986909-B2
    优先权日:2001-07-30
    标 题 :Solid phase synthesis of salts of organic acid
    发明人:VAN DYCK STEFAAN
    权利人:KEMIN IND INC
    摘要:A process for the solid-phase synthesis of salts of organic acids in a granular, free-flowing, and dust-free form particularly suited for use as animal feed additives. A liquid organic acid is applied to an inert, absorbent carrier. A solid base is then added during stirring. The acid is slowly released from the carrier preventing the fast reactions that lead to the formation of clumps. The exothermic reaction releases heat which assists in reducing the moisture content of the product.

    专利号:US-2008255359-A1
    优先权日:2005-09-28
    标题:Novel Chemical Process For the Synthesis of Quinoline Compounds
    发明人:WADE CHARLES EDWARD
    权利人:WADE CHARLES EDWARD
    摘要:Disclosed is a novel, simplified and economic process for making 3-phenylsulphonyl quinolines with an amine group at position 8 of the quinoline ring system, including 3-phenylsulfonyl-8-piperazin-1-yl-quinoline in particular, in the absence of a palladium catalyst. Also disclosed is the crystallization of polymorphic forms of 3-phenylsulfonyl-8-piperazin-1-yl-quinoline.
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    合成参考文献


    参考文献:10.1007/bf00478852
    摘要:Kanishchev MI, Korneeva NV, Shevelev SA, Fainzil'berg AA. Nitropyrazoles (review). Chemistry of Heterocyclic Compounds. 1988 Apr;24(4):353–70. doi: 10.1007/bf00478852.
    参考文献:10.1007/bf00514992
    摘要:Manaev YA, Perevalov VP, Andreeva MA, Stepanov BI. Nucleophilic substitution reactions in 4-halonitro-pyrazolecarboxylic acids. Chemistry of Heterocyclic Compounds. 1986 Mar;22(3):265–7. doi: 10.1007/bf00514992.
    参考文献:10.1134/s1023193510020011
    摘要:Lyalin BV, Petrosyan VA, Ugrak BI. Electrosynthesis of 4-bromosubstituted pyrazole and its derivatives. Russian Journal of Electrochemistry. 2010 Feb;46(2):123–9. doi: 10.1134/s1023193510020011.
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