CAS: 23327-57-3; 5-Methyl-1-Phenyl-3,4,5,6-Tetrahydro-1H-Benzo[f][1,4]Oxazocine Hydrochloride

上下游产品

(R)-5-methyl-1-phenyl-1,3,4,6-tetrahydro-2,5-benzoxaz°Cine nefopam 2-Benzoylbenzoic acid 2-benzoylbenzoyl chloridenefopam

奈福泮置于盐酸体系中,化学反应 1.5H,以79.8%的收率获得盐酸奈福泮
参考文献:黄金老了吗盐酸奈非帕姆,一种非阿片类药物和非甾体类止痛药,并且在单一溶剂中大规模生产的实用一罐合成方法
标题:黄金老了吗盐酸奈非帕姆,一种非阿片类药物和非甾体类止痛药,并且在单一溶剂中大规模生产的实用一罐合成方法
摘要:盐酸奈非帕姆因其非阿片类药物(非麻醉药)和非类固醇的作用,与阿片类和其他镇痛药相比副作用少,因此在欧洲大多数国家/地区至今一直被广泛用作镇痛药.使用单一溶剂(甲苯)在一个锅中即可完成多公斤盐酸奈福opa的合成.活性药物成分(api)的纯度达到>=99.9%,具有极好的总收率(>=79%).一锅五步合成工艺涉及从苯甲酰基苯甲酸(2)形成酰氯(3),然后进行酰胺化(4),还原(5),环化(6)和形成盐酸盐(5).1).主要优点包括:(i)使用单一溶剂;(II)每个步骤中的转化率均> 90%;(III)具有成本效益且操作简便的工艺;(iv)避免了遗传毒性杂质的形成;以及(v)一锅操作提高了总产量(>=79%).对于第一次,我们报告api的表征数据1,中间体3,4,和5,以及还可能的杂质(图5A).
Doi:10.1021/acs.Oprd.7B00228

专利信息

专利号:US-2014315720-A1
优先权日:2012-10-24
标 题 :Polysaccharide ester microspheres and methods and articles relating thereto
发明人：FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY
权利人:CELANESE ACETATE LLC
摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.

专利号:CN-101208345-B
优先权日:2005-05-25
标 题 :(S) -N-methylnaltrexone, method of synthesis and pharmaceutical use thereof