Claims
- 1. A process for preparing an .alpha.-amino-penicillin having the formula: ##STR13## wherein R is a group having the formula: ##STR14## wherein R.sub.2 is hydrogen and R.sub.3 phenyl or substituted phenyl and physiologically acceptable salts thereof, which comprises reacting a silylated 6-amino-penicillanic acid, prepared by reacting 6-amino-penicillanic acid in a dry, inert water-insoluble solvent with a dihalodialkylsilane, at a temperature at or below -20.degree. C. with at least 0.8 equivalents of a mixed anhydride prepared by reacting an amide-type Dane salt having the formula: ##STR15## wherein R is as defined hereinbefore and R.sub.1 is cyano or nitro and M is an alkali metal or a triloweralkylamine, with an alkylchlorocarbonate, in the presence of a catalyst, in methylene chloride containing as cosolvent at least 10% by volume of dimethylacetamide having a water content of 4-5%, to yield an N-protected aminopenicillin, hydrolyzing the N-protected aminopenicillin to yield an .alpha.-aminopenicillin and a .beta.-ketoamide, and recovering the .alpha.-aminopenicillin and the .beta.-ketoamide.
- 2. The process of claim 1, wherein said mixed anhydride is prepared at a temperature of -10.degree. C. or below.
- 3. The process of claim 1, wherein said catalyst is N-methylmorpholine.
Parent Case Info
This is a division of application Ser. No. 31,890, filed Apr. 20, 1979, now U.S. Pat. No. 4,231,954.
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BEX |
Divisions (1)
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Number |
Date |
Country |
Parent |
31890 |
Apr 1979 |
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