CAS: 5006-62-2; Ethyl Piperidine-3-Carboxylate

相似化合物

130250-54-3 194726-40-4 25137-01-3

上下游产品

(R)-3-哌啶甲酸乙酯 (R)-Ethyl Nipecotate 25137-01-3
1-甲基-3-哌啶甲酸乙酯 Ethyl 1-Methylpiperidine-3-Carboxylate 5166-67-6
3-哌啶甲酸 Nipecotic Acid 498-95-3
1-苄基-3-哌啶甲酸乙酯 Ethyl 1-Benzylpiperidine-3-Carboxylate 72551-53-2

(S)-Di-(Ethylnipecotate)-L-(Dibenzoyl)Tartrate Salt置于sodium Carbonate体系中,用 甲基叔丁基醚,水 作为反应溶剂,以86%的收率获得产物3-哌啶甲酸乙酯
参考文献:Development Of An Efficient Synthesis For A Nipecotate-Containing Immunopotentiator
标题:Development Of An Efficient Synthesis For A Nipecotate-Containing Immunopotentiator
摘要:The Preparation Of Elanco Animal Health Immunopotentiator (S)-Ethyl-1-(2-Thiopheneacetyl)-3-Piperidinecarboxylate (1) Is Described. The Synthesis Includes A New Resolution Of Racemic Ethyl Nipecotate With Dibenzoyl-L-Tartaric Acid. The Resolved Salt Is Found To Couple Directly With Commercially Available 2-Thiopheneacetyl Chloride Under Environmentally Friendly Schotten-Baumann Conditions To Afford The Amide In High Yield. The Final Product Is An Oil Which Is Purified By Wiped Film Evaporative Distillation.
DOI:10.1021/op049941C

专利信息

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-2011029896-A1
优先权日:2009-09-11
标 题 :Methods of preparation of muscarinic acetylcholine receptor antagonists
发明人：CARANGIO ANTONELLA; CHEUNG IZABEL; D SOUZA ERIN CARMEN FRANCES; LEAHY JOHN HENRY; STRACHAN JOHN BRYCE
权利人:GLAXO GROUP LTD; CARANGIO ANTONELLA; CHEUNG IZABEL; D SOUZA ERIN CARMEN FRANCES; LEAHY JOHN HENRY; STRACHAN JOHN BRYCE
摘要:The present application describes novel intermediates useful in the synthesis of mAChRs and methods for preparing these intermediates, comprising a compound of Formula (II): wherein, P is a suitably nitrogen protecting group; R is selected from the group consisting of C 1 - 8 alkyl, C 2 - 8 alkenyl, C 2 - 8 alkynyl, C 3 - 6 cycloalkyl, C 3 - 6 cycloalkenyl, heterocyclic, heterocyclic C 1 - 4 alkyl, aryl, aryl C 1 - 4 alkyl and heteroaryl C 1 - 4 alkyl; and Y is a suitable leaving group.

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-7511141-B2
优先权日:2001-03-02
标题 :Piperidine-piperazine ligands for neurotransmitter receptors
发明人：PERSONS PAUL E; RADEKE HEIKE
权利人:SEPRACOR INC
摘要:One aspect of the present invention relates to piperidine-piperazine compounds. A second aspect of the present invention relates to the use of the piperidine-piperazine compounds as ligands for various mammalian cellular receptors or transporters or both, including dopamine, serotonin or norepinephrine receptors or transporters, any combination of them, or all of them. 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, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, 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 piperidine-piperazine compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine receptors or transporters or both.

专利号:US-2002177721-A1
优先权日:2000-12-04
标题 :Methods for the stereoselective synthesis of substituted piperidines