CAS: 875444-08-9; (4S,5R)-5-(3,5-Bis(Trifluoromethyl)Phenyl)-4-Methyloxazolidin-2-One

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CAS号877384-16-2 [(1S,2R)-2-[3,5... | CAS号1182350-90-8 [(S)-2-(3,5-bis... | CAS号1152029-16-7 (1R,2S)-2-amino... | CAS号32315-10-9 三光气 | CAS号17352-25-9 3,5-二碘苯甲醛 | CAS号875446-37-0 安塞曲匹

Benzyl (1S)-2-[3,5-Bis(Trifluoromethyl)Phenyl]-1-Methyl-2-Oxoethylcarbamate置于aluminum Isopropoxide,Potassium Hydroxide体系中,用 异丙醇,甲苯,水 作为反应溶剂,化学反应 15.0H,以91%的收率获得产物(4S,5R)-5-(3,5-双(三氟甲基)苯基)-4-(甲基-1,3-噁唑烷-2-酮
参考文献:我们可以使小分子倾斜吗高度亲脂性taro抑制剂的优化
标题:我们可以使小分子倾斜吗高度亲脂性taro抑制剂的优化
摘要:我们描述我们的优化努力改善的物理化学性质,溶解度和脱靶轮廓1,芋头的抑制剂,在生物合成途径的壁磷壁酸(wta)合成的早期阶段酶.化合物1在酶分析中显示出125 Nm的taro Ic 50,具有很高的亲脂性(clogp = 7.1),在pbs缓冲液中没有可测的溶解度.结构-活性关系(sar)研究导致一系列化合物的亲脂性配体效率(lle)提高,与clogp的降低一致.通过这些努力,模拟9我们选择了我们最初的体内研究,与有效剂量的亚胺培南(ipm)结合可有效降低中性粒细胞减少性葡萄球菌鼠感染模型中的细菌负担.在使用9进行体内优化的同时,我们进一步改善了lle,如更多类似药物的类似物26所示.
DOI:10.1021/acs.Jmedchem.7B00113

专利信息

专利号:WO-2013091696-A1
优先权日:2011-12-21
标题 :Synthesis of intermediates for preparing anacetrapib and derivatives thereof
发明人：HUMLJAN JAN; MARAS NENAD
权利人:LEK PHARMACEUTICALS; HUMLJAN JAN; MARAS NENAD
摘要:The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.

专利号:EP-2468735-A1
优先权日:2010-12-23
标 题:Synthesis of intermediates for preparing anacetrapib and derivates thereof
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.

专利号:US-9212118-B2
优先权日:2010-12-23
标题:Synthesis of intermediates for preparing anacetrapib and derivatives thereof
发明人：HUMLJAN JAN; MARAS NENAD
权利人:HUMLJAN JAN; MARAS NENAD; LEK PHARMACEUTICALS
摘要:The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.

专利号:EP-2655348-A1
优先权日:2010-12-23
标 题 :Synthesis of intermediates for preparing anacetrapib and derivatives thereof

专利号:US-2016263565-A1
优先权日:2013-10-08
标题:Ruthenium-catalyzed synthesis of biaryl compounds in water

专利号:WO-2012085133-A1
优先权日:2010-12-23
标 题:Synthesis of intermediates for preparing anacetrapib and derivatives thereof