Organic Process Research & Development
Article
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dropwise. The suspension was centrifuged and several times
rinsed with cold water. Then the wet cake was transferred into a
Ribbon dryer. The temperature was adjusted at 50−55 °C, and
drying was performed under vacuum until the water content
reached less than 0.05%. Finally, 101.04 kg product was
obtained. Yield and purity were more than 94% and 98.5%,
respectively.
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AUTHOR INFORMATION
Corresponding Author
■
Notes
The authors declare no competing financial interest.
(26) Chou, T. S. Process for preparing desacetoxycephalosporins.
U.S. Patent 3,944,545, 1976.
ACKNOWLEDGMENTS
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(27) Sutherland, J. D.; et al. Process for the production of SSC’s via
expandase activity on penicillin G. U.S. Patent 5,919,680, 1999.
(28) Spry, D. O. J. Am. Chem. Soc. 1970, 92, 5006−5011.
(29) Alargova, R., KadiyalaI., A. Le Tiran, ZhangY., Solid forms of 1-
ethyl-3-(5-(5-fluoropyridin-3-Yl)-7-(pyridin-2-Yl)-1H-benzo[d]imida-
zol-2-Yl)urea. WIPO Pat. Appl. WO/2009/076200, 2009
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The authors are grateful to DAANA Pharmaceutical Company
for its financial support and procurement of analysis equipment
as well as bench- and pilot-scale operations.
NOMENCLATURE
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GCLE
4-methoxybenzyl-3-chloromethyl-1-7(2 phenylaceta-
mido)-3-cephem-4-carboxylate
Pen-G.K. penicillin G potassium
Ceph-C cephalosporin C
Ceph-G cephalosporin G
BSU
N,N′-bis(trimethylsilyl)urea
REFERENCES
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