CAS: 610309-89-2; 1-(9H-Carbazol-4-Yloxy)-3-[2-(2-Methoxyphenoxy)Ethylamino]Propan-2-Ol,Phosphoric Acid,Hydrate

卡维地洛置于盐酸,磷酸二氢铵体系中,用 水,乙腈 作为反应溶剂,化学反应 1.0H,反应生成 卡维地洛磷酸盐
参考文献:Efficient Process For Production Of Carvedilol Phosphate
标题:Efficient Process For Production Of Carvedilol Phosphate
摘要:一种成本效益高的新型合成磷酸盐的过程被揭示,用于合成1-(9H-咔唑-4-氧基)-3-[[2-(2-甲氧基苯氧基)乙基]氨基]-丙醇-2-醇(卡维地洛磷酸盐)的化学式(II),产率高,纯度高.更具体地,该发明揭示了一种用各种磷酸盐形成试剂(如五氧化二磷,多聚磷酸,重磷酸氢二钾,磷酸氢铵和磷酸氢钠)在丙腈,丙酮和四氢呋喃等溶剂中制备卡维地洛的结晶磷酸盐的过程.用于制备卡维地洛磷酸二氢盐溶剂的溶剂为甲醇,乙醇和异丙醇.

专利信息

专利号:US-7777053-B2
优先权日:2007-05-17
标题:Efficient process for production of carvedilol phosphate
发明人：SANGANBHATLA SHANKAR; SURYAVANSHI JITENDRA PANDURANG; ZAHID ALAM SAYYED
权利人:WANBURY LTD
摘要:A novel cost effective process for the synthesis of phosphate salts of 1-(9H-carbazol-4yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]amino]-propan-2-ol, (carvedilol phosphate) of formula (II) with high yields and purity is disclosed. More particularly, the invention discloses a process for preparation of crystalline phosphate salts of carvedilol using various phosphate forming reagents such as phosphorous pentoxide, polyphosphoric acid, dipotassium hydrogen phosphate, ammonium dihydrogen ortho phosphate, and sodium dihydrogen ortho phosphate in solvents selected from Acetonitrile, acetone and tetrahydrofuran. The solvents used to prepare solvates of carvedilol dihydrogen phosphate are methanol, ethanol and isopropyl alcohol.