CAS: 120011-70-3; 2-((1-Benzylpiperidin-4-yl)Methyl)-5,6-Dimethoxy-2,3-Dihydro-1H-Inden-1-One Hydrochloride

5,6-二甲氧基茚酮置于jones Reagent,甲酸,Palladium 10% On Activated Carbon,Potassium Iodide,Calcium Chloride体系中,用 乙醇,水,丙酮,甲苯 用作溶剂,化学反应 4.5H,反应生成盐酸多奈哌齐
参考文献:一种盐酸多奈哌齐的合成方法
标题:一种盐酸多奈哌齐的合成方法
摘要:本发明属于医药技术领域,公开了一种盐酸多奈哌齐的合成方法.以5,6‑二甲氧基‑1‑茚酮和4‑吡啶甲醛为起始原料,采用混合催化剂生成中间体i,采用氢源试剂代替氢气进行催化转移氢化反应,最后与氯化苄反应并成盐得到盐酸多奈哌齐.本发明所用催化剂通过过滤即可全部除去,后处理简单,反应条件温和,且解决了现有技术中氢气还原的选择性问题,收率和纯度均较高,适合工业化生产.

专利信息

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-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-2009253746-A1
优先权日:2005-11-14
标题 :Synthesis and Preparations of Intermediates and New Polymorphs Thereof Useful For The Preparation Of Donepezil Hydrochlcoride
发明人：SOLDEVILLA MADRID NURIA
权利人:SOLDEVILLA MADRID NURIA
摘要:The invention relates to an improved process for preparing 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyin-dan- 1 -one (a key intermediate in the synthesis of donepezil hydrochloride), crystalline polymorph forms of this key intermediate and their use thereof for producing donepezil hydrochloride. In particular, the invention provides an improved method for producing the intermediate 2-(1-benzylpiperidin-4-ylmethyliden)-5,6-dimethoxyindan-1-one. The process includes reacting 5,6-dimethoxyin-dan- 1 -one with 1-benzylpiperidine-4-carbaldehyde using potassium hydroxide in an aqueous solvent. The aqueous solvent can be a mixture of an organic solvent and water Where the organic solvent is not miscible with water, the reaction may be performed in the presence of a phase transfer catalyst.

专利号:US-2005239808-A1
优先权日:2002-05-10
标题 :Active substances for the treatment, diagnosis and prophylaxis of diseases in which abnormal protein structures occur
发明人：SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA
权利人:SCHRADER THOMAS; RIESNER DETLEV; RZEPECKI PETRA; NAGEL-STEGER LUITGARD; WEHNER MARK; KIRSTEN CHRISTIAN; MOLT OLIVER; ZADMARD REZA; ASCHERMANN KATJA
摘要:The invention on hand refers to diseases associated with abnormal protein structures, including Alzheimer's disease, Creutzfeldt-Jakob's disease, BSE and other prion-associated diseases. It is the task of the invention on hand to provide new active agents preventing the formation of amyloid plaques and to dissolve existing plaques, such agents being convenient for therapy, diagnosis and prophylaxis of diseases that are associated with abnormal protein structures. This task is performed in terms of the current invention by heterocyclic or aromatic agents with a rigid structure and a donor-acceptor-donor pattern (DAD), the latter being formed by donors and acceptors of hydrogen bridge linkages which comply with the β-sheet structure of the peptide or protein and thus fit as binding partners. The heterocyclic or aromatic agents are available at least as dimers. They recognise peptides and proteins with a β-sheet structure, form stable complexes with them and inhibit their aggregation to β-amyloid plaques. Furthermore, the new active agents are able to dissolve β-amyloid plaques that already exist. Another task of the current invention is to provide methods for the synthesis of said heterocyclic or aromatic compounds.

专利号:US-10035796-B2
优先权日:2014-08-14
标题:Crystalline forms of a BACE inhibitor, compositions, and their use
发明人：KAZAKEVICH IRINA; TRZASKA SCOTT; FENG TAO
权利人:MERCK SHARP & DOHME
摘要:The present invention provides a novel synthesis of verubecestat, and two novel crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an Aβ pathology and/or a symptom or symptoms thereof. Non-limiting examples of such Aβ pathologies, including Alzheimer's disease, are disclosed herein.

专利号:US-8063062-B2
优先权日:2006-12-20
标 题 :Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition
发明人：LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL
权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SHADID BELAL; SOLVAY PHARM BV
摘要:Embodiments of this invention relate to compounds having a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions comprising these compounds, to methods for preparing these compounds, methods for preparing novel intermediates useful for the synthesis of these compounds, and methods for preparing compositions comprising these compounds. The invention also relates to methods of treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficit disorder, traumatic brain injury, drug dependence, addiction or substance abuse by administering a pharmaceutical composition comprising these compounds to a patient in need thereof. A compound with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition is a compound of formula (1) n nwherein the symbols have the meanings given in the specification.