3-哌啶甲酸乙酯置于potassium Carbonate体系中,用 水,异丙醇 用作溶剂,化学反应生成(R)-3-哌啶甲酸乙酯 参考文献:A Practical Synthesis Of The Platelet Fibrinogen Antagonist,Elarofiban 标题:A Practical Synthesis Of The Platelet Fibrinogen Antagonist,Elarofiban 摘要:Elarofiban Is A Novel,Nonpeptide,Orally Active Fibrinogen Receptor Antagonist Useful For The Treatment Of Platelet Mediated Thrombotic Disorders (Costanzo,M. J.; Hoekstra,W. J.; Maryanoff,B. E. Wo,97/41102,1997). Herein We Describe The Process Research That Was Carried Out For The Synthesis Of Elarofiban That Eventually Led To The Development Of A Safe And Cost-Effective Commercial Scale Process. Doi:10.1021/op034103O
专利号:US-5220016-A 优先权日:1991-07-29 标 题:Synthesis of navelbine analogs 发明人:MAGNUS PHILIP D; THURSTON LEE S 权利人:UNIV TEXAS 摘要:The invention is a de novo synthesis of the norcatharanthine moiety of navelbine. The synthesis includes condensing a Grignard reagent prepared from an amine-protected R(+)-piperidinyl methanol with an N-protected 2-methoxyoxalyl indole. The indole N-protecting group is removed to provide a 2-methoxyindole hydroxy ester which is coupled to vindoline. After removal of the amineprotecting group from the piperidinyl group, ring closure to the indole moiety provides dihydrodesethyl navelbine. Other derivatives and analogs of navelbine with potential clinical applications in cancer chemotherapy may be readily synthesized. The synthesis opens a route to a wide variety of navelbine modifications, including modifications at or near the tryptamine bridge.
专利号:US-7692019-B2 优先权日:2000-12-04 标 题:Methods for the stereoselective synthesis of substituted piperidines 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HEFFERNAN MICHELE L R; HOEMANN MICHAEL Z; KESSLER DONALD W; SHAO LIMING; WU XINHE; XIE ROGER L 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
专利号:WO-2024185775-A1 优先权日:2023-03-06 标 题:Long-chain alkenyloxy–substituted benzoyl derivative and oligonucleotide synthesis method using same 发明人:OKADA YOHEI; INANAGA KAZATO; SHOJI Yukiya; MIZUFUNE HIDEYA; SUDO TATSUYA; ADACHI Sota; HOSOI Kazushi 权利人:SPERA PHARMA INC; TOKYO UNIV OF AGRICULTURE AND TECHNOLOGY 摘要:The purpose of the present invention is to provide a novel pseudo–solid phase protecting group that can be used in liquid-phase oligonucleotide synthesis. The purpose of the present invention is also to provide an oligonucleotide synthesis method that uses a novel pseudo–solid phase protecting group. The present invention provides a compound represented by formula (1) (in which R represents a C14–60 alkenyl group, n represents 2 or 3, m represents 0 or 1, p represents 1 or 2, X represents C, N, O, or S, Y represents a single bond or B(CH 2 ) t * or may form a ring with X, and Z represents a single bond or (CH 2 ) s (s being an integer from 1 to 5)). The present invention also provides an oligonucleotide production method that uses the compound.
专利号:US-7816375-B2 优先权日:2000-09-11 标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof 发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING 权利人:SEPRACOR INC 摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:US-2002177721-A1 优先权日:2000-12-04 标题 :Methods for the stereoselective synthesis of substituted piperidines
专利号:US-2006211864-A1 优先权日:2000-12-04 标题:Methods for the stereoselective synthesis of substituted piperidines
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合成参考文献
参考文献:10.1007/s11696-023-03176-6 摘要:Bhavsar S, Joshi S, Deshmukh V, Pawar S, Dond B, Mishra A, Kayastha AK, Yeole R, Deshpande P, Bhagwat S, Patel M. Design and development of an efficient convergent synthetic strategy for novel β-lactam enhancer zidebactam (WCK 5107). Chem. Pap. 2023 Nov 12;78(3):1493–504. doi: 10.1007/s11696-023-03176-6.