CAS: 54660-78-5; 4-Chloropyrimidin-5-Amine

该化合物是一种多用途的热循环化合物,其成分包括一个火利米丁骨上的氯和氨基功能组,其反应性氯米地核心能够有选择性地进行核生殖性替代反应,使其成为制药和农用化学合成中有价值的中间体.五点的地雷组的存在进一步增强了其在衍生中的用途,允许建造更复杂的分子结构.该化合物在药用化学中特别有用,有助于发展动脉抑制剂和其他生物活性分子.其定义明确的再活性和稳定性在标准条件下使它成为研究和工业应用的可靠建筑块.

结构式图片

相似化合物

5413-85-4 5177-27-5 20090-59-9

欧盟法规

ECHA物质C&L通报

上下游产品

H-pyrimidine-4-thione5-amino-6-chloro-3H-pyrimidine-4-thione 4-chloro-5-amino-6-mercaptopyrimidine H-pyrimidine-4-thione5-amino-3H-pyrimidine-4-thione 4-chloro-N-(4-chloro-5-pyrimidinyl)-3-cyanobenzamide 2-(4-chloropyrimidin-5-yl)isoindoline-1,3-dione 4-chloro-N-methylpyrimidine-5-amine

合成工艺路线路线简述

  • 合成目标产物 5-Amino-4-Chloropyrimidine 主要起始原料 5-Amino-6-Chloro-1H-Pyrimidine-4-Thione
  • (文献来源)合成步骤主要原料 5-Amino-6-Chloro-1H-Pyrimidine-4-Thione
5-Amino-6-Chloropyrimidin-4(1H)-Thione Hydrochloride置于氨体系中,用 甲醇 作为反应溶剂,以9.9%的收率获得产物5-氨基-4-氯嘧啶
参考文献:一种激酶抑制剂及其制备和应用
标题:一种激酶抑制剂及其制备和应用
摘要:本发明提供式(I)化合物,或其立体异构体,互变异构体,氮氧化物,代谢物,前药,药学上可接受的盐或溶剂合物,其在制备治疗由pim激酶介导疾病的药物或药物组合物中的应用.

专利信息


专利号:US-10131638-B1
优先权日:2018-03-12
标 题:Synthesis of AZO intermediate
发明人:CARUANA PATRICK A; STERN ALFRED G; ZAITA ALEX J; VO THAO
权利人:US NAVY
摘要:A synthesis for an azo intermediate, 5,5′-azobis(4-chloropyrimidine) is disclosed. 5,5′-azobis(4-chloropyrimidine) is a relatively stable azo compound in that decomposition does not occur until about 194° C. 5,5′-azobis(4-chloropyrimidine) is a product of oxidative dimerization of 5-amino-4-pyrimidine, which a water soluble compound. The azo intermediate is formed in an aqueous solution, but the azo intermediate is substantially insoluble in water; and as it forms it separates producing a reaction mixture that is a slurry. The azo intermediate is isolated by filtration. The azo intermediate is marginally soluble in acetone. The yield is at least 18%, and the oxidizing agent (bleach) is inexpensive, reaction conditions do not require extreme heat or cold, which taken together make the azo intermediate suitable for scaling up.

专利号:US-2002040032-A1
优先权日:2000-07-07
标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system
发明人:GLASKY MICHELLE S; LAHIRI DEBOMOY K; FARLOW MARTIN R
摘要:A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.

专利号:US-2004116453-A1
优先权日:2001-07-17
标 题 :Synthesis and methods of use pyrimidine analogues and derivatives
发明人:FICK DAVID B; FOREMAN MARK M; GLASKY ALVIN J
摘要:A pyrimidine derivative or analogue comprises an amino-substituted six-membered heterocyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y 1 )-D, where Y 1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption, or promotes blood-brain barrier penetration of the derivative or analogue. The moiety A can have two or three nitrogen atoms in the ring; typically, the moiety A is a pyrimidine moiety, with two nitrogen atoms in the ring. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.

专利号:WO-0204451-A2
优先权日:2000-07-07
标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system

专利号:US-2003055249-A1
优先权日:2001-07-17
标 题:Synthesis and methods of use of pyrimidine analogues and derivatives
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合成参考文献


参考文献:10.1016/j.jmb.2017.06.016
摘要:Georgiou C, McNae I, Wear M, Ioannidis H, Michel J, Walkinshaw M. Pushing the Limits of Detection of Weak Binding Using Fragment-Based Drug Discovery: Identification of New Cyclophilin Binders. J Mol Biol. 2017 Aug 04;429(16):2556–70. doi: 10.1016/j.jmb.2017.06.016.
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