发明名称 PROCESS FOR THE PREPARATION OF MORPHINE ANALOGS VIA THE REACTION OF ORGANOMETALLIC REAGENTS WITH AN OXAZOLIDINE DERIVED FROM MORPHINANS
摘要 <p>The oxazolidine derived from the reaction of oxymorphone with the Burgess reagent, temporarily protected at O-3 and C-6, reacts with Grignard or other suitable metallic or organometallic reagents to directly provide, for example, A/-allyl, A/-methylcyclopropyl and /V-methylcyclobutyl derivatives that are further converted into naltrexone, naloxone, nalbuphone and nalbuphine in excellent yields. These morphine analogs can be prepared from the oxazolidine in a one-pot synthesis.</p>
申请公布号 EP2809674(A1) 申请公布日期 2014.12.10
申请号 EP20130743449 申请日期 2013.01.30
申请人 BROCK UNIVERSITY 发明人 HUDLICKY, TOMAS;ENDOMA-ARIAS, MARY ANN
分类号 C07D489/08 主分类号 C07D489/08
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