摘要:
Improved processes for making opioid products having low impurity levels including making 14-hydroxycodeinone and 14-hydroxymorphinone from thebaine and oripavine, respectively.
摘要:
A morphinone reductase enzyme having the characteristics: (1) with the NADH cofactor it reduces morphinone to hydromorphone; (2) with the same cofactor it also reduces codeinone and neopinone but has no significant enzymatic activity in the reverse direction; (3) it has a molecular weight of about 81,000, as determined by gel filtration; and (4) in phosphate buffer it exhibits maximal activity at pH about 8.0.
摘要:
A process for the preparation of Tramadol according to a Grignard reaction of 2(dimethylaminomethyl)cyclo-hexanone with the reagent 3-methoxyphenylMgX, where X is a halogen, to obtain the crude base which is then introduced to a solvent, comprises contacting the crude base with hydrobromic or hydriodic acid to form a salt thereof, and subjecting the salt to a re-crystallisation step to obtain the product Tramadol hydrobromide or Tramadol hydriodide respectively, from which purified Tramadol base is obtainable for optional conversion to a pharmaceutically preferred form e.g. Tramadol hydrochloride.
摘要:
The present provides a process for preparing a compound of formula (3), the process comprising the steps of: (a) providing an aqueous acidic solution comprising a compound of formula (1) and, as an impurity, a compound of formula (2); and (b) treating the aqueous acidic solution of step (a) such that the compound of formula (2) dehydrates to form a compound of formula (1) and the compound of formula (1) is reduced to form an aqueous acidic solution of the compound of formula (3),
wherein: the treating of step (b) is carried out at one or more temperatures greater than ambient in the presence of a hydrogenation catalyst and hydrogen gas; and wherein for the compounds of formulae (1), (2) and (3): i) R 1 is -OH, R 2 is -OH and R 3 -H; or ii) R 1 is -OCH 3 , R 2 is -H and R 3 -CH 3 ; or iii) R 1 is -OH, R 2 is -H and R 3 -CH 3 ; or iv) R 1 is -OCH 3 , R 2 is -H and R 3 -H; or v) R 1 is -OH, R 2 is -H and R 3 -H; or vi) R 1 is -OCH 3 , R 2 is -OH and R 3 -H.
摘要:
A liquid hydrocarbon is rendered unpalatable by introducing thereto a denaturant suitable for discouraging the ingestion of the hydrocarbon liquid, but hitherto presenting difficulties in achieving that purpose, particularly with paraffinic liquids such as lamp oil, white spirit, kerosene and other hydrocarbon solvents, wherein the denaturant is a denatonium compound, preferably denatonium benzoate, or an analogue or derivative thereof exhibiting similar organoleptic effects, and using a sufficient amount of a liquid stabiliser miscible with said hydrocarbon liquid, e.g. an alkanol or derivative thereof, to obtain a stable solution or suspension of said denaturant in said liquid hydrocarbon.
摘要:
On effectue la synthèse de (+)-pilocarpine par l'intermédiaire de propane-1,3-diols monoprotégés homochiraux préparés dans > 98 % d'excès énantiomère par acylation catalysée enzymatiquement du diol correspondant, ainsi que des lactones dérivés, ou par l'intermédiaire d'alcools acétyléniques qui, par imidazolisation et carbonylation catalysée, sont convertis en lactones, ce qui produit encore des pilocarpines et leurs analogues.
摘要:
The present provides a process for preparing a compound of formula (3), the process comprising the steps of: (a) providing an aqueous acidic solution comprising a compound of formula (1) and, as an impurity, a compound of formula (2); and (b) treating the aqueous acidic solution of step (a) such that the compound of formula (2) dehydrates to form a compound of formula (1) and the compound of formula (1) is reduced to form an aqueous acidic solution of the compound of formula (3),
wherein: the treating of step (b) is carried out at one or more temperatures greater than ambient in the presence of a hydrogenation catalyst and hydrogen gas; and wherein for the compounds of formulae (1), (2) and (3): i) R 1 is -OH, R 2 is -OH and R 3 -H; or ii) R 1 is -OCH 3 , R 2 is -H and R 3 -CH 3 ; or iii) R 1 is -OH, R 2 is -H and R 3 -CH 3 ; or iv) R 1 is -OCH 3 , R 2 is -H and R 3 -H; or v) R 1 is -OH, R 2 is -H and R 3 -H; or vi) R 1 is -OCH 3 , R 2 is -OH and R 3 -H.
摘要:
A liquid hydrocarbon is rendered unpalatable by introducing thereto a denaturant suitable for discouraging the ingestion of the hydrocarbon liquid, but hitherto presenting difficulties in achieving that purpose, particularly with paraffinic liquids such as lamp oil, white spirit, kerosene and other hydrocarbon solvents, wherein the denaturant is a denatonium compound, preferably denatonium benzoate, or an analogue or derivative thereof exhibiting similar organoleptic effects, and using a sufficient amount of a liquid stabiliser miscible with said hydrocarbon liquid, e.g. an alkanol or derivative thereof, to obtain a stable solution or suspension of said denaturant in said liquid hydrocarbon.
摘要:
A morphinone reductase enzyme having the characteristics: (1) with the NADH cofactor it reduces morphinone to hydromorphone; (2) with the same cofactor it also reduces codeinone and neopinone but has no significant enzymatic activity in the reverse direction; (3) it has a molecular weight of about 81,000, as determined by gel filtration; and (4) in phosphate buffer it exhibits maximal activity at pH about 8.0.