CAS: 641-36-1; Apocodeine

📜Codeine置于sodium Hydride体系中,用 四氢呋喃 作为反应溶剂,化学反应 0.25H,反应生成 R(-)-阿朴可待因盐酸盐
参考文献:Aporphines. 27. Mechanistic Aspects Of The Rearrangement Of Thebaine And Codeine Analogs In Methanesulfonic Acid. Improved Method For The Synthesis Of N-Alkylated Aporphines
标题:Aporphines. 27. Mechanistic Aspects Of The Rearrangement Of Thebaine And Codeine Analogs In Methanesulfonic Acid. Improved Method For The Synthesis Of N-Alkylated Aporphines
摘要:
DOI:10.1021/jo01300A001

专利信息

专利号:US-2010216998-A1
优先权日:2007-09-18
标题:Facile 'One Pot' Process for Apomorphine From Codeine
发明人：GURUSAMY NARAYANASAMY
权利人:MALLINCKRODT INC
摘要:An improved method for producing apomorphine and derivatives thereof is provided. The method is a convenient ‘one-pot’ process, comprising the conversion of codeine into apomorphine without isolating the apocodeine intermediate. Use of water reactive scavengers, reagents that will react irreversibly with water, decreases side product formation and allows the use of milder reaction conditions. This one-pot synthesis of apomorphine from codeine provides a faster reaction with improved yields at temperatures lower as compared to conventional methods. The lower operating temperatures and less volatile reactants make the method particularly useful for large-scale manufacturing.

专利号:US-2010228032-A1
优先权日:2006-03-31
标题 :Process for Making Apomorphine and Apocodeine
发明人：GURUSAMY NARAYANASAMY
权利人:GURUSAMY NARAYANASAMY
摘要:There is provided an improved and convenient process for the synthesis of aporphines, such as apomorphine and apocodeine, by the rearrangement of the corresponding morphine or codeine derivatives. The use of a suitable water scavenger in an acid catalyzed rearrangement of the morphine derivatives unexpectedly results in a reaction temperature convenient for plant operation without sacrificing product. The method of the present invention also alleviates the cumbersome operations that were employed in the prior art to eliminate water from the reaction mixture at the elevated temperatures. This process is adaptable for the general preparation of other aporphines from the corresponding morphine congeners.