Process for preparing griseolic acid derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

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536 24, 536 26, C07D 4734, A61K 3152

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047835320

ABSTRACT:
Griseolic acid and dihydrodesoxygriseolic acid derivatives having an alkyl or aralkyl group as a substituent on the amino group at the 6-position are prepared by reacting the unsubstituted compound with a compound R.sup.7 -X (where R.sup.7 is alkyl or aralkyl and X is halogen or sulfonyloxy). The group first substitutes and quaternizes the 1-nitrogen atom. The compound is then subjected to an appropriate combination of temperature and pH to cause ring cleavage, rearrangement and ring closure involving the 6-amino group and this quaternized 1-nitrogen to give a 6-alkylamino or 6-aralkylamino derivative.

REFERENCES:
patent: 4460765 (1984-07-01), Naitr et al.
patent: 4634706 (1987-01-01), Kaneko et al.

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