CAS: 61413-54-5; 4-(3-(Cyclopentyloxy)-4-Methoxyphenyl)Pyrrolidin-2-One

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CAS号360042-78-0 tert-Butyl (+/-... | CAS号1021867-92-4 methyl 3-(3-cyc... | CAS号878210-03-8 1-benzyl-4-(3-(... | CAS号67-56-1 甲醇 | CAS号138509-45-2 4-溴-2-(环戊基氧基)苯甲醚 | CAS号569342-89-8 [2-(3-cyclopent... | CAS号85416-75-7 (−)-Rolipram | CAS号85416-73-5 (S)-(+)-咯利普兰

(+/-)-1-Benzyl-4-(3-Cyclopentyloxy-4-Methoxyphenyl)-Pyrrolidin-2-One置于氨,Lithium体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.17H,以95%的收率获得产物咯利普兰
参考文献:手性非外消旋fischer卡宾配合物与偶氮甲亚胺的首次高度区域选择性和非对映选择性[3 + 2]环加成反应:(+)-咯利普兰的对映选择性合成.
标题:手性非外消旋fischer卡宾配合物与偶氮甲亚胺的首次高度区域选择性和非对映选择性[3 + 2]环加成反应:(+)-咯利普兰的对映选择性合成.
摘要:报道了以对映选择性的方式合成1,3,4-三取代和1,4-二取代的吡咯烷-2-酮衍生物的新方法.(+/-)-薄荷醇和(-)-8-苯基薄荷醇的1,3-偶极环加成与原位产生的官能化的偶氮甲亚胺的费希尔烷氧基烯基卡宾卡宾配合物产生相应的环加合物,为螯合的四羰基菲舍尔卡宾配合物.在所有情况下仅检测到一种区域异构体,并且当使用(-)-8-苯基薄荷醇衍生的卡宾时,反应的非对映选择性非常高.环加合物的氧化和进一步转化提供了容易获得吡咯烷基-2-酮的途径.利用这种新开发的方法,可以很容易地通过四个步骤以20%的总产率制备抗炎和抗抑郁药(+)-咯利普兰.
DOI:10.1002/1521-3765(20010817)7:16<3533::Aid-Chem3533>3.0.Co;2-E

专利信息

专利号:US-9315483-B2
优先权日:2007-09-13
标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof
发明人：JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT
权利人:CONCERT PHARMACEUTICALS INC
摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.

专利号:US-2003004337-A1
优先权日:2000-05-04
标 题 :Efficient lactam synthesis
发明人：JUNG KYUNG WOON; YOON CHEOL HWAN
摘要:Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a γ-lactam, in which an a-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh 2 (OAc) 4 , n n n by which means lactams that are precursors in the synthesis of diverse natural and synthetic products, including pyrrolidinone compounds such as lactacystin, pramanicin, kainic acid, statine, AHPPA, and rolipram, are produced.

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:EP-3599246-A1
优先权日:2018-07-25
标题 :Means and methods for synthesizing precursors of y-aminobutyric acid (gaba) analogs
发明人：POELARENDS GERRIT JAN; BIEWENGA LIEUWE; VAN DER MEER JAN-YTZEN; PODDAR HARSHWARDHAN; THANGAVELU SARAVANAN
权利人:UNIV GRONINGEN
摘要:The invention relates to the fields of drug development and biocatalysis, more specifically to a biocatalytic route for asymmetric synthesis of precursors of y-aminobutyric acid (GABA) analogs. Provided is an isolated mutant 4-oxalocrototonate tautomerase (4-OT) enzyme comprising the following mutations (i) leucine at position 8 substituted with a tyrosine (L8Y) or a phenylalanine (L8F); (ii) methionine at position 45 substituted with a tyrosine (M45Y); and (iii) phenylalanine at position 50 substituted with an alanine (F50A), wherein the positions are numbered according to the amino acid sequence of 4-OT ofPseudomonas putida.Also provided is a method for the synthesis of a precursor for the pharmaceutically relevant enantiomer of a GABA analog, comprising (i) providing a y-nitroaldehyde using the 4-OT mutant enzyme, followed by (ii) subjecting the thus obtained y-nitroaldehyde to an enzymatic oxidation reaction catalyzed by an aldehyde dehydrogenase (EC 1.2.1.3).

专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

专利号:US-6689890-B2
优先权日:2000-05-04
标 题:Efficient lactam synthesis
发明人：JUNG KYUNG WOON; YOON CHEOL HWAN
权利人:UNIV SOUTH FLORIDA
摘要:Lactams, libraries of lactams, and an efficient method of synthesizing a lactam, including a gamma-lactam, in which an alpha-diazoacetamide of the general structure (I) is reacted under conditions promoting intramolecular C-H insertion, for example in the presence of a rhodium salt such as Rh2(OAc)4,by which means lactams that are precursors in the synthesis of diverse natural and synthetic products, including pyrrolidinone compounds such as lactacystin, pramanicin, kainic acid, statine, AHPPA, and rolipram, are produced.