专利号:US-2012302756-A1 优先权日:2010-02-19 标 题 :Process for synthesis of 2-substituted pyrrolidines and piperadines 发明人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 权利人:LELETI RAJENDER REDDY; LIU YUGANG; PRASHAD MAHAVIR 摘要:The present invention provides a highly efficient, versatile one-step process for asymmetric synthesis of either diastereomer of 2-substituted pyrrolidines from a single starting material with excellent yields and high diastereoselectivety. Also provided is a method for the asymmetric synthesis of both diastereomers of 2-substituted piperidines with good yields and excellent diastereoselectivety. Diasteroselectivity is controlled effectively by choice of reducing agent.
专利号:US-4782061-A 优先权日:1984-12-21 标题:Method of treating psychotropic conditions employing substituted piperazine compounds 发明人:KRUSE CORNELIS G; VAN DER HEYDEN JOHANNES A M; VAN WIJNGAARDEN INEKE; HARTOG JAN; OLIVIER BEREND 权利人:DUPHAR INT RES 摘要:The invention relates to a group of new bicyclic heteroarylpiperazine derivatives of formula 1. It was found that these compounds have interesting psychotropic in particular anti-psychotic properties. The compounds can be prepared according to methods known for the synthesis of analogous compounds.
专利号:ES-2776889-T3 优先权日:2007-03-12 标题 :Synthesis of gamma-carbolines fused to substituted heterocycle
专利号:US-5075339-A 优先权日:1989-07-28 标 题:Benzylketone phospholipase A2 inhibitors 发明人:WILKERSON WENDELL W 权利人:DU PONT MERCK PHARMA 摘要:The invention relates to benzylketone phospholipase A2 inhibitors, pharmaceutical compositions containing them, and methods of treating phospholipase A2-mediated conditions in mammals by administration of a therapeutically effective amount of such a benzylketone phospholipase A2 inhibitor. These compounds are also intermediates in the synthesis of other PLA2 inhibitors.
专利号:US-2003073681-A1 优先权日:2001-08-21 标题:2-substituted piperidines that are ligands for monoamine receptors and transporters 发明人:HAUSKE JAMES R; AQUILA BRIAN M 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, 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 heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.
专利号:US-9156840-B2 优先权日:2010-06-18 标题:D2 antagonists, methods of synthesis and methods of use 发明人:LUEHR GARY W; SUNDARAM ARATHI; JAISHANKAR PRIYADARSHINI; PAYNE PHILIP W; DRUZGALA PASCAL 权利人:ALTOS THERAPEUTICS LLC 摘要:Provided are D 2 or D 3 antagonist compounds and pharmaceutical compositions of formula I n nand pharmaceutically acceptable salts thereof, or isomers thereof, wherein R 1 , R 2 and R 3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D 2 or D 3 receptor from the compounds of the invention.
[参考文献]: Seth Y Ablordeppey, Et Al. Identification Of A Butyrophenone Analog As A Potential Atypical Antipsychotic Agent: 4-[4-(4-Chlorophenyl)-1,4-Diazepan-1-Yl]-1-(4-Fluorophenyl)Butan-1-One. Bioorg Med Chem. 2008 Aug 1;16(15):7291-301.
合成参考文献
摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026). 摘要:García-Garrido, S. E.; Presa Soto, A.; García-Álvarez, J., Science of Synthesis: Knowledge Updates, (2025) 2.