RECENT WORK ON SYNTHETIC PHARMACEUTICALS DONE BY THE RUMANIAN CHEMICAL ENTERPRISES FOR RESEARCH AND SEMI-INDUSTRIAL PRODUCTION (ICEPS INSTITUTE)
Document Type:
Collection:
Document Number (FOIA) /ESDN (CREST):
CIA-RDP80-00809A000600340092-2
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RIPPUB
Original Classification:
S
Document Page Count:
2
Document Creation Date:
December 22, 2016
Document Release Date:
August 16, 2011
Sequence Number:
92
Case Number:
Publication Date:
August 29, 1950
Content Type:
REPORT
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Sanitized Copy Approved for Release 2011/08/17: CIA-RDP80-00809A000600340092-2
I
Feb 1950
SUBJECT Scientific - Chemistry, synthetic drugs
and antibiotics
HOW '
PUBLISHED Bimonthly periodical
WHERE
PUBLISHED Bucharest
DATE
PUBLISHED
LANGUAGE
CLASSIFICATION SECRET SECRET
CENTRAL INTELLIGENCE AGENCY
INFORMATION FROM
FOREIGN DOCUMENTS OR RADIO BROADCASTS
REPORT
CD NO.
DATE OF
SUPPLEMENT TO
REPORT NO.
THIS DOCONINT CONTAINS INFORMATION AFFECTING THE NATIONAL DIFINIS
or THE UNITED STATES WITIII TNR MGNINS OF RSFIONMI ACT 90
M. S. C.. MI AND SS.AS AMIN0I0. ITS TRANSMISSION ON THE IIVII.ATIOI
Or ITS CONTENTS IN ANY MANNSN TO AN ONAUTNOIIIIO FIASCO IS FMO?
HIIITID MT LAW. ?IPRODUCTION OF THIS FORM IS P0001MIT0D.
Revista de Chimie ((Review of Chemistry), No 1, 1950.
RECENT WORK ON SYNTHETIC PHARMACEUTICALS DONE BY
THE RUMANIAN CBMICAL ENTERPRISES FOR
RESEARCH AND SEMI-IND'JS1RlAL PRODi T7 ION ttICEPS INSTITUTE)
Prof Dr Eng C. D. Nenitescu
LA Digesg
Since its inception, ICEPS 'lay played a dominant role in research and t
development in the field of synthetic pharmaceuticals introduced into pro-
duction in Rumania, The author outlines bri:.fly the difficulties which this
institute has encountered in connection with its work on synthetic pharmaceu-
ticals and medicinals. Any problems accepted by the institute must pass
through the following four phases, (a) laboratory research; (b) planning
and designing of pilot-plant installations; (c) construction of pilot-plant
installations ;nd experimentation in pilot-plant equipment accompanied, if
necessary, by changes in the original installation; (d) final designing of
the full-scale industrial installation.
As an example of the work done at ICEPS, the author mentions the fact
that full-fledged production of sulfathia.zol has been developed and illus-
trates his comments on the subject with a complete industrial flowsheet of
that production. Other synthetic pharmaceuticals introduced into production
by ICEPS comprise the sulfonamide, formothiazol; the antisyphilitics, tri-
varsol and pentarsol; the analgesics, antipyrine and pyramidon; and the
antimalarial, paludrine. The synthesis of pharmacologically active compounds
is naturally connec+ed with other branches of the synthetic organic industry
by reason of a common source of crude :,aterials and commoL intermediates,
so that work in the field o: prarmnceuticals 's conducted from that stand-
point.
The author emphasizes the two newest products tackled by ICEPS, namely,
nitrofurane (actually 5-nitro 2-furane aldehyde semicarbazone) an. chloromy-
cetin. As far as nitrofurane is concerned, a collaborator of the institute
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has developed e i.-,w and very ingenious mez:hod foi its synthesis suitable for
application on a semi-industrial and irdusc ', l scale., As regards chloromy-
cetin, little that is new could be contributed to its chemistry.
One of the syntheses of chi oromycetin star+,E, with p-nitrobenzaldehyde
and involves the use of nitromethane. This method was discarded because of
the explosive properties of nitromethane, orhich is applied here as the sodium
salt derived from it,
The second method starts with p-ritrot?oluene and has been found to yield
satisfactory results on a laboratory scale as far as preparation of small
quantities of chloromycetin for iistribution to biological research workers
is concerned. However, this :synthesis involves a reaction of p-nitrobenzoic
acid chloride with malonic acid ester (resulting in p-nitroacetophenone by
the way of a malonic ester ketone synthesis after the acyl group has been
introduced into the malonic acid ester molecule with the aid of magnesium),
bromination of the methyl group of p-nitroacet.ophenone, and other steps which
the Rumanian workers were unable to master from the technological point of
view. In view of the difficulties encoutered in that respect, the following
synthetic method was investigated!. hippuric acid-10 hippuric acid chloride--,*
introduction of the hippuric acid group into benzene by a Friedel-Crafts
synthesis condensation with formaldehyde -)nitration
This method lea to satisfactory resu't.s on the laboratory scale, but
some difficulties remain t.o be ironed out before it can be applied in full-
scale industrial production. Attempts were made to substitute acetyl
glycoooll or toluene sulfonamide N-acetic acid for hippuric acid in this syn-
thesis and the results obtained were roughly the same as with hippuric acid.
Production of chic-omycetin in quantity is being contemplated in Rumania.
As far as production of this antibiotic by the fermentation method is concerned,
the facilities of a streptomy-in plant, construction on which was started in
1945 and completed it 1948, are being utilized..
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