专利号:US-11286254-B2 优先权日:2017-10-30 标题:Process for the synthesis of 2-benzhydryl-3 quinuclidinone 发明人:DONNOLA MONICA; MOSSOTTI MATTEO; BARBERO MAURO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:The present invention discloses a process for the preparation of 2-benzhydryl-3-quinuclidinone (1). (I). The process of the invention allows to obtain the intermediate 2-benzhydryl-3-quinuclidinone (1) by reaction of 2-benzylidene-3-quinuclidinone (2) with the Grignard reagent phenyl-magnesium halide, in particular chloride or bromide, in the presence of catalytic amounts of copper (I) salts. Taking advantage of the high efficiency of the catalytic system of the copper (I) salts, 2-benzhydryl-3-quinuclidinone (1) is obtained in higher yields than those of the known processes. Advantageously, since the amounts of copper (I) salts are catalytic, the latter can easily be removed from the reaction mixture, and the process is carried out in the presence of solvents less toxic and expensive than those used in the state of the art.
专利号:US-5086179-A 优先权日:1988-04-27 标题 :Process for the preparation of optically pure amides 发明人:POWERS MATTHEW R; YOUSSEFYEH RAYMOND D; STUDT WILLIAM L; GOLEC FREDERICK A 权利人:RHONE POULENC RORER PHARMA 摘要:This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT 3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D 2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.
专利号:WO-2017072796-A1 优先权日:2015-10-30 标题 :2-pyridone based compounds useful as potential phosphodiesterase3a (pde3a)inhibitors and a process for the preparation thereof 发明人:KUMAR G JAGADEESH; MAHENDAR B; SAIDULU M; BANERJEE S K; RAO V JAYATHIRTHA 权利人:COUNCIL SCIENT IND RES 摘要:Formula A wherein X = COOCH 3 , COOC 2 H 5 , CN Y = Methyl, Phenyl R = alkyl, substituted phenyl, napthyl, furonyl, thiophenyl, substituted quinolinyl The present invention related to compounds of general FormulaA. The invention provides the synthesis of 2-pyridones useful as potential cardio tonic agents and a process for the preparation thereof.
专利号:US-2015031675-A1 优先权日:2012-02-02 标题 :Diazabicyclo[3.3.1]nonanes, methods of synthesis, and uses thereof 发明人:STRACHAN JON-PAUL; YOHANNES DANIEL 权利人:TARGACEPT INC 摘要:The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
专利号:US-8252930-B2 优先权日:2006-07-06 标 题:Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition 发明人:STOIT AXEL; COOLEN HEIN K A C; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G 权利人:STOIT AXEL; COOLEN HEIN K A C; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G; SOLVAY PHARM BV 摘要:Azaindole derivatives of formula (I): n nwherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
专利号:EP-3704116-A1 优先权日:2017-10-30 标 题 :Process for the synthesis of 2-benzhydryl-3 quinuclidinone