136232-95-6Relevant academic research and scientific papers
Preparation of 6,14-Ethenomorphinan Derivatives
Marton, J.,Hosztafi, S.,Berenyi, S.,Simon, C.,Makleit, S.
, p. 1229 - 1240 (1994)
Dihydronorthevinone (2b) was prepared from dihydrothevinone (2a) with diethyl azodicarboxylate (DEAD) and transformed into a number of new N-substituted dihydronorthevinone derivatives (2c-2g).Grignard reactions of the new compounds with methylmagnesium iodide and tert-butyl-magnesium chloride were studied.O-Demethylation of 3a-3j resulted in the corresponding N-substituted buprenorphine and diprenorphine analogs 4a-4j. - Keywords: Buprenorphine; Diprenorphine; Dihydronorthevinone; N-Substituted Dihydronorthevinone; Grignard-reactions; Morphine alkaloids; O-Demethylation with DIBAL.
Demethylation of Reticuline and Derivatives Thereof with Fungal Cytochrome P450
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, (2021/07/31)
The invention relates to recombinant host cells that expresses one or more genes encoding a cytochrome P450 enzyme capable of N-demethylating and/O-demethylating reticuline and/or derivatives thereof, and also methods of producing a N-demethylated and/or O-demethylated reticuline and/or derivatives thereof, comprising cultivating the recombinant host of the invention in a culture medium under conditions in which the one or more genes encoding the cytochrome P450 enzymes is/are expressed. The reticuline and derivatives thereof are useful for providing access to naturally unavailable and chemically difficult-to-produce starting materials for opioids.
DEUTERATED COMPOUND AND MEDICAL USE THEREOF
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, (2020/01/12)
The present invention relates to a compound represented by formula I and a non-toxic pharmaceutically acceptable salt thereof. In formula (I), R1 is H, CH3 or deuterated methyl (CD3); R2 is CH3 or CH2CH3; R3, R4 and R5 are each independently H or deuterium (D); when R1 is H or CH3, at least one of R3, R4 and R5 is D.
PREPARATION OF BUPRENORPHINE
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Paragraph 00309-00313, (2018/12/13)
Disclosed are methods for preparing buprenorphine from, for example, compounds such as nororipavine and northebaine.
PROCESS FOR THE PREPARATION OF OPIOID COMPOUNDS
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Page/Page column 43-44, (2015/11/27)
The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.
PROCESS FOR THE PREPARATION OF OPIOID COMPOUNDS
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, (2015/11/27)
The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.
AN IMPROVED PROCESS FOR THE PREPARATION OF MORPHINANE ANALOGUES
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, (2009/10/30)
The present invention relates to an improved process for preparing morphinane analogues of formula (1) wherein the substituents R1, R2, R2a, R3, R4, R5 and Y have the meanings as defined in the specifications.
PREPARATION OF OPIATE ANALGESICS BY REDUCTIVE ALKYLATION
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Page/Page column 9, (2008/06/13)
A process for preparing a compound of formula (A), (B) or (C): wherein P is H, CH3 or a hydroxyl protecting group; X is O, a protected ketone, OH, a protected hydroxyl group or H; Y is OH, a protected hydroxyl group or H; W is C(CH3)2OH, C(CH3)(C(CH3)3)OH or COCH3; Z is C2-C10 alkyl or C2-C10 arylalkyl; and ′ is a. single bond or a double bond, is disclosed. The process is a reductive alkylation in the presence of hydrogen and a reductive alkylation catalyst.
Pharmaceutical compositions for suppository
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, (2008/06/13)
A pharmaceutical composition for suppository which comprises buprenorphine or its pharmaceutically acceptable acid added salt as the active ingredient and a mixed base composed of 70 to 95 wt.% of polyethylene glycol with average molecular weight of 200 to 20,000 and 30 to 5 wt.% of propylene glycol.
