Facile N-demethylation of erythromycins

DOI: 10.1016/S0040-4039(99)00244-0

Source and publish data:

Tetrahedron Letters p. 2497 - 2500 (1999)

Update date:2022-08-11

Topics:

Authors:

Hengeveld, John E.

Gupta, Ashok K.

Kemp, Anne H.

Thomas, Albert V.

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Article abstract of DOI:10.1016/S0040-4039(99)00244-0

4_-Deoxyerythromycin B reacts with 1-chloroethyl chloroformate to give the corresponding N-demethyl N-chloroethyl carbamate. Mild methanolysis removes the chloroethyl group giving the N-demethyl erythromycin derivative while also forming the 6,9-enol ether moiety. Further manipulation gives ABT- 229, a potential prokinetic agent.

Full text of DOI:10.1016/S0040-4039(99)00244-0

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