PROCESS FOR MAKING CARBAPENEM COMPOUNDS

WIPO Patent Application WO2003027067

A3

The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by formula (I), or a salt thereof, wherein R¿1< and R¿2? are the same or different, and are selected from H, alkyl, aryl, and heteroaryl, comprising washing a carbapenem solid containing organic solvent with an organic solvent containing water; and using vacuum and/or inert gas (hydrated or dry) at low temperature to produce a compound of formula (I) containing pharmaceutically acceptable levels of organic solvents, wherein the water content of the crystalline carbapenem solid, correcting for organic solvents, is maintained at about 13% to about 25% during the process.

CVETOVICH RAYMOND (US)
WENSLOW ROBERT (US)
WILLIAMS JOHN M (US)
SIDLER DANIEL (US)
CROCKER LOUIS (US)
TUNG HSIEN-HSIN (US)
JOHNSON BRIAN K (US)
KUKURA JOSEPH II (US)
DOLLING ULF (US)

PCT/US2002/029879

September 10, 2004

September 20, 2002

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MERCK & CO INC (US)
CVETOVICH RAYMOND (US)
WENSLOW ROBERT (US)
WILLIAMS JOHN M (US)
SIDLER DANIEL (US)
CROCKER LOUIS (US)
TUNG HSIEN-HSIN (US)
JOHNSON BRIAN K (US)
KUKURA JOSEPH II (US)
DOLLING ULF (US)

C07D477/00; C07D487/04; C07D477/02; C07D477/20; (IPC1-7): C07D477/20

US20020128254A1

2002-09-12

NATISHAN ET AL.: "Residual solvents determination in the antibiotic L-749,345 by headspace gas chromatography", JOURNAL OF CHROMATOGRAPHY A, vol. 800, 1998, pages 275 - 281, XP004113603

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