Process for the preparation of cyano acetamide derivatives

C - Chemistry – Metallurgy – 07 – D

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260/103, 260/113

C07D 499/72 (2006.01) C07D 499/00 (2006.01) C07D 501/20 (2006.01)

Patent

CA 1128931

Abstract of the Disclosure Process for the preparation of acid amide derivatives of the general formula Image (I) wherein R1 represents hydrogen, or C1-6 alkyl, R2 is hydrogen, optionally a substituted aromatic or heteroaromatic preferably phenyl, furyl, thienyl, pyridyl, or optionally substituted C1-6 alkyl, preferably furylalkyl or phenylalkyl group or R1 and R2 together form alkylene, which is optionally substituted, preferably furylalkylene or phenylalkylene, R3 represents hydrogen or an easily cleavable esterifying group. preferably trialkyl-silyl or tri- chloroethyl, Image is Image or Image or Image and salts thereof by acylation of amines of the general formula II (II) Image - wherein R3 and A are as given above-which comprises reacting amines of the general formula II or salts thereof - wherein R3 and A are as defined above - with an ester of the general formula (III) Image > wherein Rl, R2 and R3 are as defined above and X is halogen, preferably chlorine or fluorine - and, if desired, splitting off the R3 protecting group of the ester group in positions 3 or 4 and/or setting free the product, if desired, from the salt thereof and/or converting it to salt. The compounds are valuable antibiotics.

307252

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