CAS: 2107-69-9; 5,6-Dimethoxy-2,3-Dihydro-1H-Inden-1-One

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(5,6-Dimethoxyindan-1-yl)Methanol置于silica Gel,Pyridinium Chlorochromate体系中,用 二氯甲烷 用作溶剂,化学反应 6.0H,以72%的收率获得5,6-二甲氧基茚酮
参考文献:使用六价铬试剂进行不寻常的 C[dbnd]C 键裂解:伯醇氧化为酮
标题:使用六价铬试剂进行不寻常的 C[dbnd]C 键裂解:伯醇氧化为酮
摘要:在二氯甲烷中用 Pdc 或 Pcc 氧化 1-羟甲基茚满和 1-羟甲基四氢萘反应生成1-茚满酮和 1-四氢萘酮.
Doi:10.1080/00397919308013800

专利信息

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-2009131535-A1
优先权日:2002-02-27
标题:Propargylamino indan derivatives and propargylamino tetralin derivatives as brain-selective mao inhibitors
发明人：BLAUGRUND ERAN; HERZIG YAACOV; STERLING JEFFREY
权利人:TEVA PHARMA
摘要:The subject invention provides derivatives of propargylamino indan (PAI) and propargylamino tetralin that selectively inhibit monoamine oxidase (MAO) in the brain, having the structure: n n n n n n n n n n wherein R 1 is OC(O)R 9 and R 2 is H,n wherein R 9 is branched or unbranched C 1 to C 6 alkyl, aryl, or aralkyl, orn nR 1 is OC(O)R 4 and R 2 is OC(O)R 4 ,n wherein R 4 is branched or unbranched C 1 to C 6 alkyl, aryl, aralkyl or NR 5 R 6 ,n wherein R 5 and R 6 are each independently H, C 1 to C 8 alkyl, C 6 to C 12 aryl, C 6 to C 12 aralkyl or C 6 to C 12 cycloalkyl, each optionally substituted; n wherein R 3 is H or C 1 to C 6 alkyl; wherein n is 0 or 1; and wherein m is 1 or 2,n nor a pharmaceutically acceptable salt thereof. Additionally, the subject invention provides methods of treating neurological disorders using these compounds, uses of these compounds for the manufacture of medicaments for treating neurological disorders and processes for synthesis of these compounds.

专利号:US-2014128613-A1
优先权日:2011-03-25
标 题:A process for preparation of intermediates of donepezil hydrochloride
发明人：GURUSAMY RENUGADEVI; ROY MITA; SHANMUGANATHAN RAMASUBRAMANIAN; JAGTAP ASHUTOSH; HARIHARAN SIVARAMAKRISHNAN; MISHRA SUSHIL KUMAR; WANKHEDE KARUNA
权利人:GURUSAMY RENUGADEVI; ROY MITA; SHANMUGANATHAN RAMASUBRAMANIAN; JAGTAP ASHUTOSH; HARIHARAN SIVARAMAKRISHNAN; MISHRA SUSHIL KUMAR; WANKHEDE KARUNA; PIRAMAL ENTPR LTD
摘要:The present invention provides a process for the preparation of key intermediate for the synthesis 5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1-indanone hydrochloride (donepezil hydrochloride). The present invention particularly provides a process for the preparation of 5,6-dimethoxy-2-(4-pyridylmethylene)-1-indanone comprising condensation of 5,6-dimethoxy-1-indanone with 4-pyridinecarboxaldehyde using an alkali metal hydroxide as a mild base in the presence of demineralized water as a solvent at a temperature in the range of 15° C. to 45° C. to yield 5,6-dimethoxy-2-(4-pyridylmethylene)-1-indanone, which is subsequently benzylated using benzyl bromide in the presence of solvent at a reflux temperature to yield 1-benzyl-4-[(5,6-dimethoxy-1-indanone-2-yl)methylene]pyridinium bromide.

专利号:AR-058187-A1
优先权日:2005-11-14
标 题 :SYNTHESIS OF AN INTERMEDIARY AND POLYMORPHIC FORMS OF THE SAME THAT ARE USED FOR THE PREPARATION OF DONEPEZYL CHLORHYDRATE.

专利号:CN-101410374-A
优先权日:2005-11-14
标题 :Improved synthesis and preparation of intermediates for the preparation of donepezil hydrochloride and new polymorphs thereof

专利号:EP-1960357-A2
优先权日:2005-11-14
标 题 :Synthesis and preparations of intermediates and polymorphs thereof useful for the preparation of donepezil hydrochloride