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Naloxone nalorphine and naltrexone are examples of

Posted Apr 21, 2016 by Admin

Percodan (17) and numorphan (16) are also available by N-methylation of compounds (18) and (19 respectively, using standard methods. Noroxymorphone (19) is a centrally important precursor for naloxone (20 naltrexone (21) nalmefene (22 all valuable narcotic antagonists in the natural stereochemical series (Chart 3).Catalytic hydrogenation of compound (13) (generally with palladium) smoothly affords crude nearly pure noroxycodone (18) in quantitative yield. Addition of formaldehyde in this hydrogenation provides the clinically used agonist percodan (17). Hydrogenation of (14) to (15) followed by N-methylation of (15) gives (28) the same intermediate to Foxy. The potent narcotic antagonist cyclofoxy (30 when labeled with 18F, was recently shown to be a highly useful agent for labeling opiate receptors in the living brain by.

TOTAL SYNTHESIS OF NORTHEBAINE, NORMORPHINE, NOROXY ORPHONE ENANTIOMERS AND DERIVATIVES VIA N-NOR INTERMEDIATES Field of the Invention The present invention relates to a total synthesis proceeding from nordihydrocodeinone (4) as in the post scheme, and a key aspect is that a facile method has now.Since both - and (-)-nordihydro codeinone are equally available by the earlier Rice patents, the present disclosure is applicable and pertains to synthesis of compounds of both the natural (-)- and unnatural -stereochemical series.

Alternately, O-demethylation of (15) to 14-hydroxydihydronormorphine (27) followed by N-cyclo- butylation gives nalbuphine. The potent narcotic agonist Foxy which is useful in pharmacological studies can also be obtained (Chart 5) from (-)-(14) by hydrogenation in the presence of formal dehyde to (28 previously converted to.Oxidation of northe- baine (12) with performic acid formed in situ afforded pure 14-hydroxynorcodeinone (13) in 90 yield after crystallization from any short chain alcohol, such as methanol or other suitable purification technique.

This compound is easily available from (15) by N-cyclopropylation to (31) which is O-demeth- ylated to the corresponding 6 -naltrexol 32 and treated as previously described by prior art. Alternately, conversion of (27) to the N-cyclopropylmethyl derivative affords the same intermediate naltrexol.Conversion can also be accomplished by addition of a strong base, such as potas- sium t-butoxide, or other organic base. Treatment of the enol ether (10) in a short chain alcohol such as methanol with halogenating reagent, preferably a brominating reagent such as N-bromoacetamide and.

The process is shorter and more flexible than total synthesis through thebaine and is also applicable to synthesis of the unnatural opiate series (not available from opium deriva- tives some members of which are potent antitussives.Applicability of the Pr).

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For example, treatment of northebaine with cyclopropylmethylbromide gives cyclo- propylmethylnorthebaine (33 an intermediate useful for synthesis of buprenorphine (34 a state of the art agonist antagonist drug which is effective by sublingual administration.Previously, the naltrexol was prepared by borohydride reduction of naltrexone and required chromatographic fractionation to remove the corresponding 6-B-isomer. An additional utility of the instant invention is that it renders N-alkylnorthebaines including thebaine (8) readily available by total synthesis in either the natural or unnatural.

Summary The instant invention is a process in which nordihydrocodeinone (4 an early intermediate in the total synthesis of codeine, morphine and thebaine. Chart 1, is converted through intermediate without substituents on nitrogen to a number of versatile N-nor intermediates.Background Previous Rice patents, US 4,368,326 and 4,521,601, disclose the total synthesis of either enantiomer of nordihydrocodeinone (4) and the subsequent conversion of this compound to the N-methyl derivative, dihydrocodeinone (5 which is a useful intermediate in this context for synthesis of codeine (6 morphine.

A major disadvantage of the commercial process is the multistep removal of N-methyl group involving the acylation reaction, reaction with cyanogen bromide or phosgene-derived chloroformate (which are toxic and otherwise dangerous reagents), and the hydrolysis step.For example, in the synthesis of the narcotic antagonists, natural thebaine is sequentially oxidized to 14-hydroxy- codeinone, reduced to 14-hydroxydihydrocodeinone, 0- demethylated to oxymorphone. The methyl group is then removed by the following sequence: acetylation to the 3,14-diacetoxy derivative, reaction with cyanogen bromide or a.

N-alkylation of compound (19) with allyl or cyclopropylemthyl bromide by standard methods gives naloxone and naltrexone, respectively. These compounds can also be obtained (Chart 3) by alkyla- tion of noroxycodone (18) to compounds (23) and (24 followed by O-demethylation with BBr3 or other suitable reagent.This results in a shorter and more economical process by eliminating a substantial number of steps and requirements for labor and raw materials. Furthermore, each step in the process gives very high yields and each isolated intermediate is obtained pure, or very nearly so, by.

The potent antagonist diprenorphine (35) can also be prepared from N-cyclopropylmethylnorthebaine by prior art procedures which were demonstrated only in the natural stereochemical series. It is thus clear that the instant invention is an extremely practical thebaine-free total synthesis of all clinically used 14-hydroxymorphinans and.For total synthesis, the instant invention thus differs from the prior art by not utilizing thebaine, that is, it is unnecessary to introduce the methyl group (4 5, Chart 1) and then remove it after further transforma tion of thebaine.

Reaction of naltrexone (21) with methylene triphenylphosphorane according to standard protocol then gives nalmefene (22). Stereoselective reduction of 14- hydroxynorcodeinone (13) generally with any stereoselec tive reduction agent, preferably an alkali borohydride such as sodium borohydride, gives 14-hydroxynorcodeine (14) to the exclusion of the isocodeine.These compounds can serve as precursors for a number of important drugs (with the natural opiate stereochemistry) currently used in the practice of medicine. The process thus eliminates the need for thebaine for the total synthesis of these drugs.

The latter three compounds are the only raw materi- als obtained from opium which are of value in the produc tion of narcotics, narcotic antagonists and the agonist- antagonist drugs. In the standard manufacturing process of the narcotic antagonists, naloxone (20 naltrexone (21 nalmefene (22.The hydrolysis of the N-cyano employed in the standard process requires prolonged heating with a large excess of 25 sulf ric acid that results in partial destruction of the desired noroxymorphone.

O-Demethylation of percodan (17) by standard procedures gives numorphan (16) also used clini cally as a potent narcotic agonist. Brief treatment (0- demethylation) of compound (18) with BBr3 or other stan dard O-demethylation procedure then gives noroxymorphone (19).(-)- Codeine has also been advanced as a possible starting material for these compounds. Since both natural thebaine and codeine have a methyl substituent on the nitrogen, removal of the methyl group and replacement with a cyclo- alkylmethyl or allyl group and other structural alter.