Process for Producing Methyl-morphin (Codein), Ethyl-morphin, and Higher Homologues of Morphin.
Year: 1886

page_text: Date of Application, 13th Aug., 1886.
Complete Left, 23rd Apr., 1887.
Complete Accepted, 27th May, 1887.
Process for Producing Methyl-morphin (Codein), Ethyl-morphin,
and Higher Homologues of Morphin.
1, ALBERT KNOLL, Doctor of Philosophy of Ludwigshafen on the Rhine, Germany,
do hereby declare the nature of this invention to be as follows:-
My process for obtaining the higher homologues of morphin is based on the heating
of morphin, or of a compound of morphin and alkali or earthy alkali, with methyl-
ethyl etc. sulphates, which causes the alkyl radical of the latter to enter the morphin-
molecule in place of an atom of hydrogen or of metal.
This transformation with the production of morphin-homologues takes place in
aqueous as well as in alcoholic solution, and in working with or without pressure.
"For instance, to produce methyl-morphin or codein, I dissolve one part of morphin
in two parts of alcohol of 90% strength, add sufficient potash or soda-lye to dissolve
the whole quantity of morphin, introduce into this solution methyl-sulphate of potash
or of soda, either in the calculated proportions or an excess, and heat for two hours
with the use of a return flow cooler in the water bath, whereby codein is formed and
the liquid becomes brown and turbid.
The separation or precipitation of the codein and the recovery of undecomposed
morphin are effected by well known processes; for instance, by neutralising with
sulphuric acid, relieving of alcohol, diluting with water, precipitating the morphin
with ammonia, and separating by filtration, dissolving the codein by the addition of
benzol and stirring, and further isolating and purifying as is usual in the case
of alkaloids.
In an analogous manner I proceed for the production of other homologues of
morphin.
FAIRFAX & WETTER,
433. Strand, London,
Agents for the Applicant.

page_text: and Higher Homologues of Morphin.
I, ALBERT KNOLL, Doctor of Philosophy, of Ludwigshafen on the Rhine, Germany,
do hereby declare the nature of my invention for PROCESS FOR PRODUCING METHYL-
MORPHIN (CODEÏN), ETHYL-MORPHIN AND HIGHER HOMOLOGUES OF MORPHIN, and in
what manner the same is to be performed, to be particularly described and ascertained
in and by the following statement :-
My process for obtaining the higher homologues of morphin is based on the heating
of morphin or of a compound of morphin and alkali or earthy alkali with ethyl-
methyl etc., sulphates which causes the alkyl radicle of the latter to enter the morphin-
molecule in place of an atom of hydrogen or of metal. This transformation with the
production of morphin-homologues takes place in aqueous as well as in alcoholic
solution, and in working with or without pressure.
For instance, to produce methyl-morphin or codein, I dissolve one part of morphin
in two parts of alcohol of 90% strength, add sufficient potash or soda lye to dissolve
the whole quantity of morphin, introduce into this solution methyl-sulphate of potash
or of soda, either in the calculated proportions or an excess, and heat for two hours
with the use of a return flow cooler in the water bath, whereby codein is formed and
the liquid becomes brown and turbid.
The separation or precipitation of the codeïn and the recovery of undecomposed
morphin are effected by well-known processes, for instance by neutralising with
sulphuric acid, relieving of alcohol, diluting with water, precipitating the morphin
with ammonia, and separating by filtration, dissolving the codein by the addition of
benzol and stirring, and further isolating and purifying as is usual in the case
of alkaloids.
In an analogous manner I proceed for the production of other homologues of
morphin.
Having now particularly described and ascertained the nature of my said invention,
and in what manner the same is to be performed, I declare that what I claim is:
1. The process for the production of methyl-morphin (codeïn), ethyl-morphin and
higher homologues of morphin, which consists in causing the corresponding sulphate
(that is to say, the methyl-, or ethyl- etc. sulphate) to act on an alkaline solution of
morphin, or of morphin-alkali, or of the morphin-compound of an earthy alkali.
2. Obtaining methyl-morphin (codeïn), ethyl-morphin, or a higher homologue of
morphin in the manner substantially as described.
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