CAS: 57-29-4; (4R,4Ar,7S,7Ar,12Bs)-3-Prop-2-Enyl-2,4,4A,7,7A,13-Hexahydro-1H-4,12-Methanobenzofuro[3,2-E]Isoquinoline-7,9-Diol,Hydrochloride

专利信息

专利号:US-5668285-A
优先权日:1986-10-31
标 题 :Total synthesis of northebaine, normophine, noroxymorphone enantiomers and derivatives via N-Nor intermediates
发明人：RICE KENNER CRALLE; NEWMAN AMY HAUCK
权利人:US HEALTH
摘要:The invention involves a method of making key intermediates useful in the synthesis of many opiate narcotics and antagonists and agonists; and the non-opiate enantiomers thereof which have potent antitussive properties. The synthesis starts from either the natural or unnatural enantiomer of nordihydrocodeinone and produces 8, 14-dihydronorthebaine, the diketal of 7-bromonordihydrocodeinone, northebaine, norcodeinone diketal and 14-hydroxynorcodeinone intermediates without the necessity of leaving the N-nor structure. The syntheses have fewer steps than previous methods, and also have high yields.

专利号:EP-0496830-B1
优先权日:1989-10-16
标 题 :Total synthesis of northebaine, normorphine, noroxymorphone enantiomers and derivatives via n-nor intermediates
发明人：RICE KENNER CRALLE; NEWMAN AMY HAUCK
权利人:US HEALTH
摘要:Families of antagonist-agonists and opiate narcotics are produced from norhydrocodeinone. In a preferred embodiment, norhydrocodeinone is refluxed with sulfosalicyclic dimethylketal and delta-6-enol ether derivatives and is then converted entirely to the ether by the addition of dry tetrahydrofuran simultaneously with the removal of the thus produced ether. The ether is then reacted with methanesulfonic acid and N-bromoacetamide to form the hydrobromide salt of the 7-bromodimethylketal derivative. From this derivative, a variety of products can be derived, including the novel further intermediate 14 hydroxynorcodeinone. The present invention enables derivation using a starting material which, unlike the starting materials of prior art processes, is available in the natural (-) or synthetic (+) form. Thus, the method of the present invention provides the only known route for the synthesis of (+) forms of various derivatives and intermediates, such as (+)-7-bromo-dimethylketal nordihydrocodeinone.

专利号:US-2012282255-A1
优先权日:2011-04-07
标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence
发明人：PLUCINSKI GREG
权利人:PLUCINSKI GREG
摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.

专利号:WO-9105768-A1
优先权日:1989-10-16
标 题:Total synthesis of northebaine, normorphine, noroxymorphone enantiomers and derivatives via n-nor intermediates

专利号:EP-0496830-A1
优先权日:1989-10-16
标 题 :Total synthesis of northebaine, normorphine, noroxymorphone enantiomers and derivatives via n-nor intermediates

专利号:EP-0496830-A4
优先权日:1989-10-16
标题:Total synthesis of northebaine, normorphine, noroxymorphone enantiomers and derivatives via n-nor intermediates