Acylation of amines

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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540221, 540225, 540227, 540314, C07D50106, C07D49912

Patent

active

053590570

ABSTRACT:
There is described a process for the manufacture of carboxylic acid amides by acylating amines with 2-benzothiazolyl thioesters of carboxylic acids, which process comprises reacting the amine in the form of an acid addition salt. This process is especially of great advantage when the amine is not particularly stable in the form of the free base, which is frequently the case especially with 7-aminocephalosporin derivatives. 7-Acylamino-cephalosporin derivatives can be manufactured in good yield and in high purity with the novel process.

REFERENCES:
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patent: 4593022 (1986-06-01), Labeeuw et al.
patent: 4641819 (1986-09-01), Nagai et al.
patent: 4716227 (1987-12-01), Furlenmeier
patent: 4767852 (1988-08-01), Ascher
patent: 4826972 (1989-05-01), Prager
patent: 4868294 (1989-09-01), Brundidge et al.

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