4-氯吡咯并嘧啶置于20% Pd(Oh)2 On Carbon 甲酸铵体系中,用 甲醇 用作溶剂,化学反应 2.0H,以97%的收率获得7H-吡咯并[2,3-D]嘧啶 参考文献:Azaindole Derivatives With A Combination Of Partial Nicotinic Acetyl-Choline Receptor Agonism And Dopamine Reuptake Inhibition 标题:Azaindole Derivatives With A Combination Of Partial Nicotinic Acetyl-Choline Receptor Agonism And Dopamine Reuptake Inhibition 摘要:阿扎因多ール衍生物的公式(i)如下: 其中符号的含义如说明书中所给.这些化合物具有部分尼古丁乙酰胆碱受体激动作用和去甲肾上腺素再摄取抑制作用.本发明还涉及包含这些化合物的药物组合物,制造它们的方法,制造用于其合成的新的中间体的方法,制造组合物的方法以及这些化合物和组合物的用途,例如,用于将它们施用于患者以在尼古丁受体和/或去甲肾上腺素转运体涉及的疾病中实现治疗效果,或者可以通过操纵这些受体来治疗的疾病.
专利信息
专利号:US-9388131-B2 优先权日:2011-04-27 标题:Automated synthesis of small molecules using chiral, non-racemic boronates 发明人:BURKE MARTIN D; LI JUNQI; GILLIS ERIC P 权利人:UNIV ILLINOIS 摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
专利号:US-10961273-B2 优先权日:2016-08-16 标 题 :N-carboxyanhydride-based-scale synthesis of elamipretide 发明人:DUNCAN SCOTT M; OUDENES JAN; ANDERSEN MARC W 权利人:STEALTH BIOTHERAPEUTICS CORP 摘要:Disclosed are methods of making elamipretide (MTP-131), a peptide compound with therapeutic potential for treating various mitochondrial myopathies. The synthesis of the peptide can be achieved via the use of N-carboxyanhydride-modified amino acid residues, which increases the efficiency of the synthetic process and the purity of the peptide product generated.
专利号:US-10683318-B2 优先权日:2014-10-17 标 题:Scalable synthesis of reduced toxicity derivative of amphotericin B 发明人:BURKE MARTIN D; UNO BRICE E; RAKSHIT SOUVIK 权利人:UNIV ILLINOIS 摘要:Disclosed is a simplified, readily scalable series of individual methods that collectively constitute a method for the synthesis of C2′epiAmB, an efficacious and reduced-toxicity derivative of amphotericin B (AmB), beginning from AmB. Also provided are various compounds corresponding to intermediates in accordance with the series of methods.
专利号:US-11897914-B2 优先权日:2021-11-29 标题 :Synthesis of 2′ protected nucleosides 发明人:POON WING C; ZOU RUIMING; LAU ALDRICH N K; YU DAVID; Du Gengyu; YAO YUN-CHIAO; ZHAO GANG 权利人:HONGENE BIOTECH CORP 摘要:Embodiments of the present application relate to the preparation of 2′-O-protected nucleoside phosphoramidites and conjugation of the 2′-O-protected nucleoside to a solid support. More specifically, the present application relates to nucleosides having a hydroxy protecting group at the 2′ position that reduces migration to the 3′ position during RNA (e.g., mRNA) synthesis and can be readily removed under mild conditions without the use of toxic metal-containing reagents. Methods of using the nucleosides described herein in RNA synthesis are also disclosed.
专利号:US-8309716-B2 优先权日:2005-07-29 标题 :Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis 发明人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J 权利人:RUGGERI SALLY GUT; HAWKINS JOEL M; MAKOWSKI TERESA M; RUTHERFORD JENNIFER L; URBAN FRANK J; PFIZER 摘要:This invention relates to methods and intermediates useful for the synthesis of pyrrolo[2,3-d]pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
参考文献:10.1016/s0960-894x(02)00042-2 摘要:Srikanth K, Debnath B, Jha T. QSAR study on adenosine kinase inhibition of pyrrolo[2,3-d]pyrimidine nucleoside analogues using the hansch approach. Bioorganic & Medicinal Chemistry Letters. 2002 Mar;12(6):899–902. doi: 10.1016/s0960-894x(02)00042-2. 参考文献:10.1016/j.bmcl.2004.04.040 摘要:González MP, Moldes del Carmen Terán M. A TOPS-MODE approach to predict adenosine kinase inhibition. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3077–9. doi: 10.1016/j.bmcl.2004.04.040. 参考文献:10.1016/j.bmc.2008.03.027 摘要:Caballero J, Fernández M, González-Nilo FD. A CoMSIA study on the adenosine kinase inhibition of pyrrolo[2,3-d]pyrimidine nucleoside analogues. Bioorg Med Chem. 2008 May 01;16(9):5103–8. doi: 10.1016/j.bmc.2008.03.027. 参考文献:10.1107/s1600536810020179 摘要:Gainsford GJ, Fröhlich RFG, Evans GB. 7-(5-Methylsulfanyl-β-D-erythrofuranosyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine monohydrate (MT-tubercidin·H2O). Acta Crystallogr E Struct Rep Online. 2010 Jun 18;66(7):o1688–9. doi: 10.1107/s1600536810020179. 参考文献:10.1007/s10637-010-9394-6 摘要:Deng M, Huang H, Jin H, Dirsch O, Dahmen U. The anti-proliferative side effects of AEE788, a tyrosine kinase inhibitor blocking both EGF- and VEGF-receptor, are liver-size-dependent after partial hepatectomy in rats. Invest New Drugs. 2011 Aug;29(4):593–606. doi: 10.1007/s10637-010-9394-6.