CAS: 1404559-15-4; ((2S,4R)-4-(4-(3-Methyl-1-Phenyl-1H-Pyrazol-5-yl)Piperazin-1-yl)Pyrrolidin-2-yl)(Thiazolidin-3-yl)Methanone
该化合物是一种主要用作抗糖尿病剂的制药化合物,具体用于管理2型糖尿病,属于Dipeptididyl peptidase-4(DPP-4)抑制剂,该抑制剂通过提高内分泌激素水平发挥作用,从而增加胰岛素分泌,并以依赖葡萄糖的方式降低葡萄素水平.这有助于降低血液凝糖水平.该化合物的特点是其特定的立体化学学,其特点是2S,4R)配置,这对它的生物活动至关重要.Teneliglilippin 展示了良好的口服生物利用率,通常以平板形式进行.其致癌性特征包括中度半衰期,允许一次性服用.此外,该化合物具有有利的安全性特征,其常见的副作用是温和可控性.该化合物还因其在体重管理和糖尿病病人心血管健康方面的潜在好处而得到注意.
- 英文名称((2S,4R)-4-(4-(3-Methyl-1-Phenyl-1H-Pyrazol-5-yl)Piperazin-1-yl)Pyrrolidin-2-yl)(Thiazolidin-3-yl)Methanone
- 中文名称[(2S,4R)-4-[4-(3-甲基-1-苯基-1H-吡唑-5-基)-1-哌嗪基]-2-吡咯烷基]-3-噻唑烷基甲酮
- IUPAC名称((2S,4R)-4-(4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl)pyrrolidin-2-yl)(thiazolidin-3-yl)methanone
- 其它别名Teneligptin Api; ((2S,4R)-4-(4-(3-Methyl-1-Phenyl-1H-Pyrazol-5-yl)Piperazin-1-yl)Pyrrolidin-2-yl)(Thiazolidin-3-yl)Methanone; Teneligliptin (2S,4R)-Isomer; [(2S,4R)-4-[4-(5-Methyl-2-Phenylpyrazol-3-yl)Piperazin-1-Yl]Pyrrolidin-2-Yl]-(1,3-Thiazolidin-3-yl)Methanone; 3-{(2S,4R)-4-[4-(3-Methyl-1-Phenyl-1H- Pyrazol-5-yl)Piperazin-1-Yl]Pyrrolidin -2-Yl-Carbonyl}Thiazolidine; Methanone, [(2S,4R)-4-[4-(3-Methyl-1-Phenyl-1H-Pyrazol-5-yl)-1-Piperazinyl]-2-Pyrrolidinyl]-3-Thiazolidinyl-; Teneligliptin 2S,4R; Teneligliptin (2S,4R)-Isomer Impurity
- CAS编号1404559-15-4
- MFCD编号:MFCD28387194
- FDA UNII编号:H8U6Z2QCB3
- 分子式:C22H30N6OS分子量:426.59
- 产品CID: 624832
- 产品分类分析化学 → 标准品 → 药典标准品和杂质标准品
物理性质
MSDS等安全信息
上下游产品
N-tert-butoxycarbonyl-L-cis-4-hydroxyproline (2S,4S)-1-(tert-butoxycarbonyl)-4-((tert-butyldimethylsilyl)oxy)pyrrolidine-2-carboxylic acid 3-[(2S,4S)-1-tert-butoxycarbonyl-4-tert-butyldimethylsiloxy-2-pyrrolidinylcarbonyl]-1,3-thiazolidine 3-((2S,4S)-1-tert-butoxycarbonyl-4-hydroxy-2-pyrrolidinylcarbonyl)-1,3-thiazolidine合成工艺路线路线简述
📜(2S,4S)-1-(Tert-Butoxycarbonyl)-4-((Tert-Butyldimethylsilyl)Oxy)Pyrrolidine-2-Carboxylic Acid置于2,6-二甲基吡啶,四丁基氟化铵,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,Trifluoromethanesulfonic Acid Anhydride,三氟乙酸体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 30.0H,反应生成特力利汀原料药
参考文献:Teneligliptin(3-[(2 S,4 S)-4-[4-(3-Methyl-1-Phenyl-1 H-Pyrazol-5-Yl)piperazin-1-Yl] Pyrrolidin-2的发现和临床前研究-基羰基]噻唑烷):一种高效,选择性,持久和口服活性的二肽基肽酶iv抑制剂,用于治疗2型糖尿病
标题:Teneligliptin(3-[(2 S,4 S)-4-[4-(3-Methyl-1-Phenyl-1 H-Pyrazol-5-Yl)piperazin-1-Yl] Pyrrolidin-2的发现和临床前研究-基羰基]噻唑烷):一种高效,选择性,持久和口服活性的二肽基肽酶iv抑制剂,用于治疗2型糖尿病
摘要:二肽基肽酶iv(dpp-4)抑制是低血糖的低风险,因此是每日一次口服给药方案的合适机制.我们在研究1-脯氨酰咪唑烷的过程中,探索了在脯氨酸结构的γ位上取代的连接的双环杂芳基哌嗪.这些努力导致发现了一种高效,选择性,持久和口服活性的dpp-4抑制剂3-[(2 S,4 S)-4-[4-(3-甲基-1-苯基-1)h-吡唑-5-基)哌嗪-1-基]吡咯烷-2-基羰基]噻唑烷(8G),具有独特的结构,具有五个连续的环.X射线共晶体结构为8G在dpp-4中的研究表明,吡唑上的苯环和dpp-4的s 2广泛的亚位点之间的关键相互作用不仅提高了效力,而且还提高了选择性.0.03 Mg / Kg或更高剂量的化合物8G在口服zucker脂肪大鼠体内后,显着抑制了血浆葡萄糖水平的增加.在日本,化合物8G(替利格列汀)已被批准用于治疗2型糖尿病.
Doi:10.1016/j.Bmc.2012.08.012
海关参考信息
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2912110000-甲醛
2912120000-乙醛
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专利信息
专利号:WO-2015173779-A1
优先权日:2014-05-16
标题:Process for the preparation of teneligliptin and its novel intermediates
发明人：DUBEY SUSHIL KUMAR; KUMAR NEERAJ; NARWAL SURESH; DUBEY SHAILENDRA KUMAR; KUMAR PRAMOD
权利人:MICRO LABS LTD
摘要:The present invention relates to a novel process for the preparation of Teneligliptin or its pharmaceutically acceptable salts and its hydrates thereof. The invention also relates to novel intermediates used in the synthesis of Teneligliptin and their preparation.
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
参考标题: Process For The Preparation Of Teneligliptin And Its Novel Intermediates Procédé De Préparation De Teneliglipin Et Nouveaux Intermédiaires Correspondants摘要:The Present Invention Relates To A Novel Process For The Preparation Of Teneligliptin Or Its Pharmaceutically Acceptable Salts And Its Hydrates Thereof. The Invention Also Relates To Novel Intermediates Used In The Synthesis Of Teneligliptin And Their Preparation.
合成参考文献
参考文献:10.1016/j.bmc.2012.08.012
摘要:Yoshida T, Akahoshi F, Sakashita H, Kitajima H, Nakamura M, Sonda S, Takeuchi M, Tanaka Y, Ueda N, Sekiguchi S, Ishige T, Shima K, Nabeno M, Abe Y, Anabuki J, Soejima A, Yoshida K, Takashina Y, Ishii S, Kiuchi S, Fukuda S, Tsutsumiuchi R, Kosaka K, Murozono T, Nakamaru Y, Utsumi H, Masutomi N, Kishida H, Miyaguchi I, Hayashi Y. Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem. 2012 Oct 01;20(19):5705–19. doi: 10.1016/j.bmc.2012.08.012.
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