CAS: 134564-82-2; (5R)-5-(Methoxymethyl)-3-[4-[(3R)-4,4,4-Trifluoro-3-Hydroxybutoxy]Phenyl]-1,3-Oxazolidin-2-One

上下游产品

3-(4-Hydroxyphenyl)-5-(Methoxymethyl)Oxazolidin-2-One 73422-62-5
(R)-3-(4-羟基苯基)-5-(甲氧基甲基)-2-恶唑烷酮 (R)-3-(4-Hydroxyphenyl)-5-(Methoxymethyl)Oxazolidin-2-One 79038-60-1
(R)-3-(4-(Benzyloxy)Phenyl)-5-(Methoxymethyl)Oxazolidin-2-One

📜(R)-3-(4-(Benzyloxy)Phenyl)-5-(Methoxymethyl)Oxazolidin-2-One置于5%-Palladium/activated Carbon,氢气,Potassium Carbonate体系中,用 乙醇,二氯甲烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 18.0H,反应生成贝氟沙通
参考文献:Practical Synthesis Of 4,4,4-Trifluorocrotonaldehyde: A Versatile Precursor For The Enantioselective Formation Of Trifluoromethylated Stereogenic Centers Via Organocatalytic 1,4-Additions
标题:Practical Synthesis Of 4,4,4-Trifluorocrotonaldehyde: A Versatile Precursor For The Enantioselective Formation Of Trifluoromethylated Stereogenic Centers Via Organocatalytic 1,4-Additions
摘要:报道了4,4,4-三氟巴豆醛(1)的实际合成及其在不对称1,4-加成反应中的应用.通过有机催化剂催化的1,4-加成反应,1与多种亲核试剂如杂芳香化合物,烷硫醇和醛肟反应,生成了各自带有高光学纯度的三氟甲基化手性中心的相应产物.其中一个产物被转化为mao-A抑制剂贝氟沙酮.
Doi:10.1039/c2Cc32757K

专利信息

专利号:WO-2008084057-A1
优先权日:2007-01-10
标题:Compounds with a combination of cannabinoid-cb1 antagonism and serotonin reuptake inhibition
发明人：LANGE JOSEPHUS H M; KRUSE CORNELIS G
权利人:SOLVAY PHARM BV; LANGE JOSEPHUS H M; KRUSE CORNELIS G
摘要:This invention relates to compounds with a combination of cannabinoid-CB1antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.

专利号:US-7354923-B2
优先权日:2001-08-10
标 题 :Piperazine melanocortin-specific compounds
发明人：SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
权利人:PALATIN TECHNOLOGIES INC
摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure: n nand stereoisomer and pharmaceutically acceptable salts thereof, where X is CH 2 or Câ•?O, R 1 , R 2 , and R 3 are as described in the specification, preferably where R 3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R 3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

专利号:WO-2005102340-A1
优先权日:2003-05-30
标题 :Piperazine melanocortin-specific compounds
发明人：SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
权利人:PALATIN TECHNOLOGIES INC; SHARMA SHUBH D; SHI YI-QUN; WU ZHIJUN; RAJPUROHIT RAMESH
摘要:Melanocortin receptor-specific piperazine or ketopiperazine compounds having the structure (I); and stereoisomer and pharmaceutically acceptable salts thereof, where X is CH2 or C=O, R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group, a second amino acid residue or a second amino acid residue with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

专利号:US-8138174-B2
优先权日:2007-01-10
标 题:Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition
发明人：LANGE JOSEPHUS H M; KRUSE CORNELIS G
权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SOLVAY PHARM BV
摘要:Compounds with a combination of cannabinoid CB 1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. n In at least one embodiment, the invention relates to compounds of the general formula (1): n nwherein the substitutents have the definitions given in the specification.

专利号:US-9751877-B2
优先权日:2012-09-21
标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
发明人：PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
权利人:PFIZER
摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

专利号:EP-0736606-B1
优先权日:1995-04-07
标题:Process for the enzymatic preparation of intermediates for the synthesis of befloxatone