FIELD: organic chemistry, chemical technology, antibiotics.
SUBSTANCE: invention relates to a method for preparing derivative of 9-deoxo-9a-aza-9a-homoerythromycin A of the formula (Ia)
or its pharmaceutically acceptable salt. Method involves interaction of compound of the formula (2)
monohydrate with n-propylamine in isopropanol medium at temperature 50-55 C and under atmospheric pressure. Method for preparing compound of the formula (2) involves the following steps: (a) transformation of compound of the formula (3)
trifluoroacetate to a free base of compound of the formula (3) wherein R4 represents hydroxy-protecting group; (b) interaction of indicated free base of compound of the formula (3) with sulfonium methylide ion; (c) quenching mixture from the stage (b) with weak acid aqueous solution and distribution of product in non-aqueous layer; (d) removal of protecting group in product from the stage (c). Invention provides enhancing yield and improved purity of end products.
EFFECT: improved preparing method.
5 cl, 6 ex
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