Processes for the preparation of 5,6-di-hydropyrrolo[2,3-d]pyrimidines
AssigneeEli Lilly and Company
InventorsCharles J. Barnett, Thomas M. Wilson
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Abstract
This invention relates to intermediates and processes thereto, for the preparation of 5,6-dihydropyrro[2,3-d]pyrimidines which are useful for the treatment of susceptible neoplasms.
Claims10
A process for preparing a 5,6-dihydropyrrolo-[2,3-d]pyrimidine of the formula ##STR15## wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl;
- or a salt thereof, which comprises
- (a) reacting a compound of formula II ##STR16## wherein R is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted;
- and
- R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl;
- or a salt thereof, with a sulfurization agent;
- and
- (b) cyclizing the reaction product from step (a) with guanidine.
A process for preparing a compound of the formula ##STR17## wherein R.sup.1 is H, C.sub.1 -C.sub.4 Alkyl, phenyl which may be substituted or benzyl;
- or a salt thereof, which comprises cyclizing a compound of formula IV ##STR18## wherein R.sup.1 is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted;
- and
- R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, phenyl which may be substituted or benzyl;
- or a salt thereof with guanidine.
A process for preparing a 5,6-dihydropyrro[2,3-d]pyrimidine of the formula ##STR19## wherein R.sup.1 is H, which comprises
- (a) reacting a compound of the formula ##STR20## wherein R is C.sub.1 -C.sub.4 alkyl or phenyl which may be substituted;
- and
- R.sup.1 is t-butyl, with a sulfurization agent;
- (b) treating the reaction product from step (a) with a strong acid;
- and
- (c) cyclizing the reaction product from step (b) with guanidine.
Dependencies are inferred from the claim text.