Process for preparing purine derivatives and intermediates there

Details Process for preparing purine derivatives and intermediates there Process for preparing purine derivatives and intermediates there

1990-04-09

1992-12-29

Rivers, Diana G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

544244, 544264, 544265, 544271, 544276, 544277, C07D47326, C07D47318, C07D47340

Patent

active

051752883

ABSTRACT:
A process for preparing pharmaceutically active compounds of formula (A): ##STR1## wherein X is hydrogen, hydroxy, chloro, C.sub.1-6 alkoxy or phenyl C.sub.1-6 alkoxy; and R.sub.a and R.sub.b are hydrogen, or acyl or phosphate derivatives thereof, which process comprises the preparation of an intermediate of formula (I): ##STR2## wherein R.sub.1 is C.sub.1-6 alkyl, or phenyl C.sub.1-6 alkyl in which the phenyl group is optionally substituted; R.sub.2 is hydrogen, hydroxy, chlorine, C.sub.1-6 alkoxy, phenyl C.sub.1-6 alkoxy or amino; and R.sub.3 is halogen, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, azido, an amino group or a protected amino group, via the reaction of a compound of formula (II): ##STR3## wherein R.sub.2 and R.sub.3 are as defined for formula (I) with: (a) a compound of formula (III): ##STR4## wherein R.sub.4 and R.sub.5 are independently hydrogen, C.sub.1-6 alkyl, or phenyl, or R.sub.4 and R.sub.5 together are C.sub.5-7 cycloalkyl; or

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Padgett, et al., J. Org. Chem., vol. 44, No. 20, pp. 3492-3496 (1979).
Csendes, et al., J. Org. Chem., vol. 44, No. 23, pp. 4173-4178 (1979).

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