专利号:US-7825244-B2 优先权日:2005-06-10 标题:Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis 发明人:BAINDUR NAND; GAUL MICHAEL DAVID; KREUTTER KEVIN DOUGLAS; XU GUOZHANG 权利人:JANSSEN PHARMACEUTICA NV 摘要:The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula C: n nwherein R 1 , R 2 , R 99 , and X are as defined herein, the use of such compounds in the synthesis of protein tyrosine kinase inhibitors, particularly inhibitors of FLT3 and/or c-kit and/or TrkB.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-8697876-B2 优先权日:2010-04-02 标 题:Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists 发明人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN 权利人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN; COLUCID PHARMACEUTICALS INC 摘要:The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).
专利号:US-7524963-B2 优先权日:2001-10-15 标题:Synthesis of (4-bromophenyl)(4-piperidyl)methanone-(Z)-O-ethyloxime and salts 发明人:WONG GEORGE S K; PARK JEONGHAN; TONG WEIDONG; RAGHAVAN RAMANI R 权利人:SCHERING CORP 摘要:In one embodiment, the present invention describes the synthesis of (4-bromophenyl) (4-piperidyl)methanone-(Z)-O-ethyloxime and its acid salts, and similar compounds, in high stereochemical purity.
专利号:US-9475837-B2 优先权日:2011-12-23 标题 :Process for the synthesis of therapeutic peptides 发明人:HURLEY FIONN; WEGNER KATARZYNA; FOLEY PATRICK 权利人:IPSEN MFG IRELAND LTD 摘要:The present invention relates to a process for the large-scale synthesis of therapeutic peptides using a Sieber Amide resin, which comprises solid-phase Fmoc-chemistry.
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
[参考文献]: Falch E, Et Al. Gaba-Mimetic Activity And Effects On Diazepam Binding Of Aminosulphonic Acids Structurally Related To Piperidine-4-Sulphonic Acid. J Neurochem. 1985 Jan;44(1):68-75. [参考文献]: Krehan D, Et Al. Phosphinic, Phosphonic And Seleninic Acid Bioisosteres Of Isonipecotic Acid As Novel And Selective Gaba(C) Receptor Antagonists. Neurochem Int. 2003 Jun;42(7):561-5. [参考文献]: Iris Thondorf, Et Al. Three-Dimensional Quantitative Structure-Activity Relationship Analyses Of Substrates Of The Human Proton-Coupled Amino Acid Transporter 1 (Hpat1). Bioorg Med Chem. 2011 Nov 1;19(21):6409-18. [参考文献]: Jing Yuan, Et Al. Genetic Mapping Of Targets Mediating Differential Chemical Phenotypes In Plasmodium Falciparum. Nat Chem Biol. 2009 Oct;5(10):765-71. [参考文献]: Phedias Diamandis, Et Al. Chemical Genetics Reveals A Complex Functional Ground State Of Neural Stem Cells. Nat Chem Biol. 2007 May;3(5):268-73.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Hou, W.; Yang, G.; Xu, H., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 158. 摘要:Hou, W.; Yang, G.; Xu, H., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 176. 参考文献:10.1007/s12033-011-9402-x 摘要:Thiele A, Stangl GI, Schutkowski M. Deciphering enzyme function using peptide arrays. Mol Biotechnol. 2011 Nov;49(3):283–305. doi: 10.1007/s12033-011-9402-x. 参考文献:10.1007/s11307-014-0748-x 摘要:Padakanti PK, Zhang X, Li J, Parsons SM, Perlmutter JS, Tu Z. Syntheses and Radiosyntheses of Two Carbon-11 Labeled Potent and Selective Radioligands for Imaging Vesicular Acetylcholine Transporter. Molecular Imaging and Biology. 2014 May 30;16(6):765–72. doi: 10.1007/s11307-014-0748-x.