Process for the preparation of a disubstituted 2,5-diamino-3-hyd

Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acid esters

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564164, 548469, 548491, 546 98, C07C26100, C07C23300, C07D20904

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active

056544669

ABSTRACT:
Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or
R.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; or
R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

REFERENCES:
patent: 2784228 (1957-03-01), Hartung
patent: 5142056 (1992-08-01), Kempf et al.
patent: 5354866 (1994-10-01), Kempf et al.
Stuk, T. et al J. Org. Chem (1994), 59(15) 4040-1.
Ghosh, et al., J. Org. Chem. 58 1025 1993.
Brillon, et al., J. Org. Chem. 57 1838 (1992).
Stuk, et al., J. Org. Chem. 59 4040-4041 (1994).

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