专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-6207858-B1 优先权日:1999-03-03 标 题 :Regioselective synthesis of DTPA derivatives 发明人:CHINN PAUL; GYORKOS ALBERT; LABARRE MICHAEL J; RUHL STEVE; RYSKAMP THOMAS 权利人:IDEC PHARMA CORP 摘要:The present invention provides a process for high yield regioselective synthesis of DTPA derivatives that eliminates the need for ion exchange chromotographic separation of intermediates. Moreover, as this process yields a single regioisomer of the chelate, it provides for the regiospecific synthesis of desired chelates useful as radiolabeling agents.
[参考文献]: Abby R Jennings, Et Al. Multifunctional Thiols From The Highly Selective Reaction Of Mercaptoalcohols With Chlorosilanes. Chem Commun (Camb). 2013 Apr 28;49(33):3467-9. [参考文献]: Adam Fekete, Et Al. Presynaptic T-Type Ca2+ Channels Modulate Dendrodendritic Mitral-Mitral And Mitral-Periglomerular Connections In Mouse Olfactory Bulb. J Neurosci. 2014 Oct 15;34(42):14032-45. [参考文献]: Ana R Ribeiro, Et Al. Microbial Degradation Of Pharmaceuticals Followed By A Simple Hplc-Dad Method. J Environ Sci Health A Tox Hazard Subst Environ Eng. 2012;47(13):2151-8. [参考文献]: Carlos Barea, Et Al. Antiplasmodial And Leishmanicidal Activities Of 2-Cyano-3-(4-Phenylpiperazine-1-Carboxamido) Quinoxaline 1,4-Dioxide Derivatives. Molecules. 2012 Aug 7;17(8):9451-61. [参考文献]: Eglal Adelhamid Abdelaleem, Et Al. Validated Chromatographic And Spectrophotometric Methods For Analysis Of Some Amoebicide Drugs In Their Combined Pharmaceutical Preparation. Pak J Pharm Sci. 2013 Jan;26(1):175-83.
合成参考文献
摘要:Stephenson, G. R., Science of Synthesis Knowledge Updates, (2014) 1, 230. 摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 408. 摘要:Heydt, H., Science of Synthesis Knowledge Updates, (2014) 3, 409. 摘要:Margaretha, P., Science of Synthesis Knowledge Updates, (2010) 4, 415. 摘要:Sang, J.; Zhang, G., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 787.