Process for an anthracycline derivative, and an anthracyclinone

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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260365, C07H 1524

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045646740

ABSTRACT:
A process for producing an anthracycline derivative represented by the general formula: ##STR1## where R.sup.1 is an acyl group, each of X.sup.1 and X.sup.2 is a hydrogen atom, a methoxy group, a hydroxyl group, a halogen atom or a lower alkyl group, each of Y.sup.1 and Y.sup.2 is a hydrogen atom, an alkoxy group or a hydroxyl group, and Z is a hydrogen atom or a protected hydroxyl group, which comprises reacting an anthracyclinone derivative represented by the general formula: ##STR2## where R is a hydrogen atom or a trialkylsilyl group, and X.sup.1, X.sup.2, Y.sup.1, Y.sup.2 and Z are as defined above, with a 1-acyl-sugar derivative represented by the general formula: ##STR3## where R.sup.2 is an acyl group and R.sup.1 is as defined above, in the presence of a silyl sulfonic acid derivative represented by the general formula:

REFERENCES:
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patent: 4161480 (1979-07-01), Pappo et al.
patent: 4348388 (1982-09-01), Garland et al.
Acton et al., "J. Med. Chem.", vol. 17, No. 6, 1974, pp. 659-660.
El Khadem et al., "Carbohydrate Research", vol. 101, 1982, C1-C4.
El Khadem, "Academic Press", 1982, pp. 221, 265.
Monneret et al., "Academic Press", 1982, pp. 225-251.

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