Osaka University

Kanegafuchi Kagaku Kogyo Kabushiki Kaisha

Minoru Hatanaka

Toshiyasu Ishimaru

Yasutsugu Shimonishi

Hisayuki Sakurai

Optically active .beta.-amino acid derivatives and their salts of the following formula: ##STR1## wherein COOR.sup.1 is an esterified or unesterified carboxyl group; R.sup.2 is hydrogen or a C.sub.1-10 acyl or esterified carboxyl group and processes for producing the same. These compounds permit important intermediate for the synthesis of 1.beta.-methylcarbapenem derivatives to be produced in an efficient way.

Optically active .beta.-amino acid derivatives and their salts, and

6-Aminoacylamidopenicillanic acid or 7-aminoacylamidocephalosporanic acids are produced in high yields by acylating 6-aminopenicillanic acid or 7-aminocephalosporanic acid with an amino acid, or a functional equivalent thereof, having its amino group protected with N,N-disubstituted .beta.-keto acid amide, and then removing the protecting group from the resulting protected 6-aminoacylamidopenicillanic acid or protected 7-aminoacylamidocephalosporanic acid by hydrolysis.

Acylation of 7-aminocephalosporanic acids

6-Aminoacylamidopenicillanic acid or 7-amino-acylamidocephalosporanic acids are produced in high yields by acylating 6-aminopenicillanic acid or 7-aminocephalosporanic acid with an amino acid, or a functional equivalent thereof, having its amino group protected with N,N-disubstituted .beta.-keto acid amide, and then removing the protecting group from the resulting protected 6-aminoacylamidopenicillanic acid or protected 7-aminoacylamidocephalosporanic acid by hydrolysis.

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Takatsuki, Japan

Minoru Hatanaka