Process for 1-carba(dethia)cephalosporins

C - Chemistry – Metallurgy – 07 – D

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C07D 463/16 (2006.01) C07D 205/085 (2006.01) C07D 463/00 (2006.01) C07F 7/10 (2006.01)

Patent

CA 1338785

The invention provides a free radical process for preparing 1-carba(1-dethia)cephalosporin antibiotics with 2-substituted methylcephalosporin 1,1- dioxides wherein the substituent on the 2-methylene group is a free radical precursor group such as a phenyl or alkylseleno group. The latter dioxides are treated with a free radical initiator, e.g., a trialkyl- tin hydride or actinic radiation at 40°C to 150°C to provide the 1-carba-3-cephem and 1-carba-2-cephem products. The invention also provides free radical compounds formed as intermediates in the process.

611402

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