Process for the preparation of .alpha.-6-deoxy-tetracyclines
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United States of America Patent
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Jul 1, 1986
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N/A
app pub date -
Aug 17, 1984
filing date -
Aug 17, 1983
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Expired
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Abstract
A process for the preparation of .alpha.-6-deoxy-tetracyclines by the stereoselective heterogeneous hydrogenation of a 6-demethyl-6-deoxy-6-methylene-tetracycline or an acid addition salt thereof, in the presence of a tertiary phosphine, or the simultaneous dehalogenation and stereo-selective heterogeneous hydrogenation of an 11a-halo-6-demethyl-6-deoxy-6-methylene-tetracycline or an acid addition salt thereof, in the presence of a tertiary phosphine, characterized by the use of a rhodium salt catalysts, wherein the rhodium is bonded to a polysiloxane carrier, having the following formulae: Rh Cl.sub.3 [N{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.3 ].sub.10 Rh Cl.sub.3 [N{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.3 ].sub.12 Rh Cl.sub.3 [N{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.3 ].sub.15 Rh Cl.sub.3 [HN{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.2 ].sub.4 Rh Cl.sub.3 [HN{(CH.sub.2).sub.3 SiO.sub.3/2 }.sub.2 ].sub.8 permitting easy recovery of the rhodium, by simple filtration.
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