Process for the production of N.sup.6 -substituted adenosine nuc

Details Process for the production of N.sup.6 -substituted adenosine nuc Process for the production of N.sup.6 -substituted adenosine nuc

1975-08-27

1978-05-16

Brown, Johnnie R.

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

Organic compounds

Carbohydrates or derivatives

424180, 536 24, C07H 1920

Patent

active

040900215

ABSTRACT:
N.sup.6 -substituted adenosines of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are a hydrogen atom or an alkyl, aralkyl, aryl or heterocyclic ring, or R.sub.1 is a hydrogen atom and R.sub.2 is hydroxy, amino, alkyl terminally substituted, or R.sub.1 and R.sub.2 collectively with the nitrogen atom are a heterocyclic ring; R.sub.3 is a hydrogen atom, amino or silylated amino; and Z is a phosphoric acid esterified sugar radical; possess antiproliferative activity and have beneficial effects upon the cardiovascular system; are produced by reacting a 6-trialkylsilyloxy purine of the formula ##STR2## wherein each alkyl are alike; R.sub.3 ' is a hydrogen atom or trialkyl silylamine; and Z' is a sugar radical blocked with a phosphoric acid ester group, with ammonia or a primary or secondary amine, or with a corresonding salt of the amine, employing the amine salt or a Lewis acid as reaction catalyst.

REFERENCES:
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patent: 3298923 (1967-01-01), Banno et al.
patent: 3413283 (1968-11-01), Nomura et al.
patent: 3590029 (1971-06-01), Koch et al.
patent: 3708469 (1973-01-01), Vorbruggen et al.
patent: 3891623 (1975-06-01), Vorbruggen et al.
patent: 3983104 (1976-09-01), Vorbruggen

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