CAS: 43088-67-1; 4-Chloro-5-Methylthieno[2,3-D]Pyrimidine

该化合物是热循环化合物,其特点是其引信的硫诺和丙酰胺环,具有独特的化学特性;4位置的氯原子和5位置的甲基组的存在,增强了其在各种有机溶剂中的回活动性和溶性;该化合物一般表现出黄色到浅棕色的表面,并因其在医药化学中的潜在应用而闻名,特别是作为研制药物的木头;其结构允许各种替代反应,使其在有机合成中成为多功能的中间体;此外,硫诺和丙胺糖糖可以影响生物活动,使其对农业化学和治疗剂的发展产生兴趣,与许多乙酰环一样,它可能在NMR和IR光谱中表现出具体的光谱特性,有助于其在实验室环境中的识别和定性;由于化学性质和潜在的生物活动,应当遵守安全和谨慎措施.

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上下游产品

CAS号43088-64-8 5-甲基-3,4-二氢噻吩并[... | CAS号19786-56-2 4-肼基-5-甲基噻吩基嘧啶 | CAS号917907-37-0 2-[(5-methylthi... | CAS号917908-06-6 3-ethoxy-4-[(5-...

合成工艺路线路线简述

  • 合成目标产物 4-Chloro-5-Methylthieno[2,3-D]Pyrimidine 主要起始原料 3-Methylthieno(2,3-D)Pyrimidin-4(5H)-One
  • (文献来源)合成步骤主要原料 3-Methylthieno(2,3-D)Pyrimidin-4(5H)-One
📜2-氨基-4-甲基-噻吩-3-羧酸乙酯置于n,N-二甲基苯胺,三氯氧磷体系中,化学反应 3.0H,反应生成 4-氯-5-甲基噻吩并[2,3-D]嘧啶
参考文献:Acoh介导的cc键形成反应超声辅助合成4-(1H-吲哚-3-基)噻吩并[2,3-D]嘧啶衍生物
标题:Acoh介导的cc键形成反应超声辅助合成4-(1H-吲哚-3-基)噻吩并[2,3-D]嘧啶衍生物
摘要:通过4-氯噻吩并[2,3-D]嘧啶与吲哚范围.该反应使用acoh作为促进剂以及溶剂进行,以非常好到可接受的收率得到相应的产物.这种无金属方法通过cc键形成反应进行,具有条件简单,持续时间短,使用环保能源等优点.除了其缺点之外,还通过合成的化合物的药用价值展示并举例说明了该方法的有用性.化合物3I和3J在体外表现出非常好的tnf-α抑制作用,被确定为初始命中分子.
DOI:10.1016/j.Tetlet.2023.154784

专利信息


专利号:US-2004138238-A1
优先权日:2002-08-08
标题 :Substituted aminopyrimidine compounds as neurokinin antagonists
发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; KESAVAN VENKITASAMY; SHARADENDU ANURAG; MOHANTY PRADYUMNA; CHEN DONGLI; CHERUKU SRINIVASA RAO; HEIFETZ ALEXANDER; KALID ORI; MARANTZ YAEL; NUDELMAN RAPHAEL; SBACHAM SHARON; BAR-HAIM SHAY
摘要:The invention discloses tachykinin receptor antagonists. The tachykinin family of receptors comprising the neurokinins substance P (SP), neurokinin A, and neurokinin B and related neuropeptides that are widely distributed in the peripheral and central nervous system. The invention discloses novel aminopyrimidine derivatives, synthesis and uses thereof for the treatment of diseases mediated directly or indirectly by the tachykinin receptors. These diseases include central nervous system disorders such as anxiety, pain, depression, emesis, in particular cancer chemotherapy induced emesis, respiratory and inflammatory bowel disease and other gastric disorders, asthma, schizophrenia, ophthalmic diseases such as glaucoma, ocular hypotension, neural injury, stroke, cardiac disorders, psoriasis, and migraine. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

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合成参考文献


参考文献:10.1007/bf00765112
摘要:Kaplina NV, Grinev AN, Bogdanova GA, Alekseeva LM, Pushkina TV, Fomina AN, Shvedov VI. Synthesis of mono- and dibromomethyl derivatives of thieno[2,3-d] pyrimidines. Pharmaceutical Chemistry Journal. 1987 Feb;21(2):126–9. doi: 10.1007/bf00765112.
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