3,5-二碘-L-酪氨酸置于氢碘酸,溶剂黄146,二异丙胺,甲胺,Sodium Hydroxide体系中,用 甲醇,水,正丁醇 作为反应溶剂,化学反应 12.0H,反应生成 甲状腺素 参考文献: Novel Process For The Preparation Of Levothyroxine Sodium[fr] Nouveau Procédé Pour La Préparation De Lévothyroxine Sodique 标题: Novel Process For The Preparation Of Levothyroxine Sodium[fr] Nouveau Procédé Pour La Préparation De Lévothyroxine Sodique 摘要:该发明提供了一种新型工艺,用于制备高纯度左旋甲状腺素钠,即(S)-2-氨基-3-[4-(4-羟基-3,5-二碘苯氧基)-3,5-二碘苯基]丙酸钠盐,通过两个工艺中间体,即3,5-二碘l-酪氨酸铜络合物和新型双(对甲氧基苯基)碘化物.该发明还提供了不含基因毒性杂质的左旋甲状腺素五水合物,以及甲状腺素水平低于0.04%重量/重量.
专利号:US-5549974-A 优先权日:1994-06-23 标题:Methods for the solid phase synthesis of thiazolidinones, metathiazanones, and derivatives thereof 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:The invention provides an efficient and versatile method for the combinatorial synthesis and screening of libraries of 4-thiazolidinones, metathiazanones, and derivatives thereof. In order to expediently synthesize a combinatorial library of derivatives based upon these core structures, a general methodology for the solid phase synthesis of these derivatives is also provided. Arrays of thiazolidinones, metathiazanones, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antihistaminic, or antimicrobial activity or use in the treatment of inflammation, hypertension, renal failure, congestive heart failure, uremia and other conditions can be prepared using this method.
专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2021130409-A1 优先权日:2017-09-01 标 题 :Method for the Solid-Phase Synthesis of Cyclic Pentapeptides 发明人:ZHENGGUO JIANG; LUCIANO FORNI; ROBERTSON ALAN 权利人:Alsonex Pty Ltd 摘要:A method for the synthesis of a cyclic ornithine-proline-D-cyclohexylalanine-tryptophan-arginine pentapeptide of Formula A; n n n n n n n n n n n n wherein R 1 and R 2 are, independently, —H, or —C(O)R 3 where R 3 is —CH 2 Ph, —CH 2 CH 2 Ph, —CHâ•?CHPh, —C(NHAC)CH 2 Ph;n nthe method comprising the steps of;n nforming a linear proline-D-cyclohexylalanine-tryptophan-arginine-ornithine pentapeptide of Formula B, attached to a polymeric resin;n n n n n n n n n n n n n n n n n wherein R 1 is as for Formula A, RES indicates the polymeric resin, and P 1 and P 2 are protecting groups;n ncyclising the linear pentapeptide of Formula B to form a cyclic pentapeptide of Formula C, attached to the polymeric resin;n n n n n n n n n n n n n n n cleaving the cyclic peptide of Formula C from the resin providing a cleaved cyclic pentapeptide having a free amine group of an ornithine residue;n noptionally substituting the free amine group of the ornithine residue of the cleaved cyclic peptide;n nremoving the protecting groups P 1 and P 2 , to providethe cyclic peptide of Formula A.
专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-9868783-B2 优先权日:2013-07-04 标 题:Inhibition of the synthesis of beta-app or the activity of the A-β peptide in the choroid plexus 发明人:DI NARDO ARIEL; MOYA KENNETH LEE; ARNAUD KAREN; PROCHIANTZ ALAIN 权利人:CENTRE NAT RECH SCIENT; COLLEGE FRANCE; INSTITUT NATIONAL DE LA SANTE ET DE LA RECH MEDICALE (INSERM); INST NAT SANTE RECH MED 摘要:The invention relates to the treatment of neurodegenerative diseases, in particular Alzheimer's disease, by inhibition of the synthesis of βAPP or of the activity of the Aβ peptide in the choroid plexus.
1: Metry M, Yusuf ARS, Lane J, Unwala R, Altisheh R. Urticarial Vasculitis Associated With Levothyroxine. Cureus. 2023 Jun 21;15(6):e40754. doi: 10.7759/cureus.40754. 2: Alofi RM, Alrohaily LS, Jan RA, Alsaedi SL, Mahrous FA, Alreefi MM. Adherence to Levothyroxine Treatment Among Patients With Hypothyroidism in Madinah, Saudi Arabia: A Cross-Sectional Study. Cureus. 2023 Jun 20;15(6):e40686. doi: 10.7759/cureus.40686. 3: Duntas LH. Focusing on the critical role of age and sex in the diagnosis of subclinical hypothyroidism and associated levothyroxine prescription. Thyroid. 2023 Jul 20. doi: 10.1089/thy.2023.0340. Epub ahead of print. 36(2):2233039. doi: 10.1080/14767058.2023.2233039. 29(7):581-588. doi: 10.1016/j.eprac.2023.04.003. 29(7):572-580. doi: 10.1016/j.eprac.2022.12.013. 32(3):727-731.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198