摘要:
The present invention is directed to an improved process for the preparation of methylphenidate, stereoisomer, mixture of stereoisomers and pharmaceutically acceptable salts thereof, more particularly, the sulfate and hydrochloride salts of methylphenidate, di-threo-methylphenidate and dexmethylphenidate. Methods of removing or reducing the amount of impurities from the above described process are also disclosed.
摘要:
The present invention is directed to processes for preparing oxycodone base having less than 10 ppm of 14-hydroxycodeinone, oxycodone hydrochloride having less than 50 ppm of 14-hydroxycodeinone, and oxycodone hydrochloride having less than 75 ppm of 14-hydroxycodeinone.
摘要:
The present invention is directed to a process for using n-butanol to prepare an oxycodone base compositions having reduced levels of impurities such as 14-hydroxycodeinone and DHDHC.
摘要:
Hydrocodone bitartrate forms are disclosed which are useful as analgesic agents either in combination with or as replacements for hydrocodone bitartrate.
摘要:
There is disclosed a process which comprises the steps of:
(a) reacting a di(hydrocarbyl)tin oxide such as a dialkyltin oxide with a dihydric alcohol, alkanolamine, or an enolizable α-hydroxy ketone in an inert organic reaction vehicle, with removal of water, at a temperature and for a period of time sufficient to produce a cyclic adduct of said dialkyltin oxide and said dihydric alcohol, alkanolamine, or enolizable α-hydroxy ketone; (b) reacting said cyclic adduct product of Step (a) with sucrose in an inert organic reaction vehicle such as a dipolar aprotic liquid, at a temperature and for a period of time sufficient to produce a 6-O-[dihydrocarbyl(hydroxy- or amino- or oxohydrocarbyl)stannoxyl]sucrose; and (c) reacting the product of Step (b) with an acylating agent to produce a sucrose-6-ester.
摘要:
The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.
摘要:
Sucrose is reacted with a 1,3-di(hydrocarbyloxy)-1,1,3,3-tetra(hydrocarbyl)distannoxane to produce a 1,3-di-(6-O-sucrose)-1,1,3,3-tetra(hydrocarbyl)distannoxane, which can be acylated to produce a sucrose-6-ester.
摘要:
A process for the chlorination of sucrose-6-esters to produce 6′,4,1′-trichlorosucrose-6-esters which comprises the steps of:
(a) adding at least seven molar equivalents of an acid chloride to a reaction mixture containing a sucrose-6-ester and a tertiary amide to form initially a chloroformiminium chloride salt which subsequently forms a complex with the hydroxyl goups of the sucrose-6-ester; (b) subjecting the reaction mixture product of step (a) to an elevated temperature not higher than about 85°C for a period of time sufficient to produce a mixture of chlorinated sucrose-6-ester products consisting essentially of 6′-chlorosucrose-6-ester, 4,6′-dichlorosucrose-6-ester, and 1′,6′-dichlorosucrose-6-ester; and (c) subjecting the reaction mixture product of step (b) to an elevated temperature not higher than about 125°C for a period of time sufficient to produce a chlorinated product consisting essentially of 1′,4,6′-trichlorosucrose-6-ester.