Synthesis of Some Steroidal [3,2-d]- and [17,16-d]-2',6'- Diaminopyrimidines

Biological activity in steroids possessing nitrogen atoms: recent advances

“…The examples involving a 5-membered heterocyclic ring embrace steroidal [3,2-b]-pyrroles (Orr & Bowers, 1962), [16,17-b]-pyrroles (Mueller & Jiu, 1961), [3,2-b]-and [3,4-b]-indoles (Doorenbos & Wu, 1962), [3,4-c]-pyrazoles (Clinton & others, 1961(Clinton & others, , 1962, [17,16-c] (Hassner & Haddadin, 1962a). Those involving a six-membered ring include [ 17,1641-pyridines (Ketcheson & Taurins, 1960, [3,2-d]-pyrimidines (de Ruggieri & others, 1962a;de Ruggieri & others, 1963c;Smith, Teller & Foell, 1963 ;Zderic & others, 1963), [17,16-d (Hassner & Haddadin, 1962b), the preparation of this last group as potential anti-tumour agents being inspired by earlier reports (Buu-Hoi & Cagniant, 1944) of haemolytic properties in quinolino-steroids. An example involving a seven-membered ring is afforded by an androsteno [17,16-e]-l,Zdiazepin-4-0ne (Moore & Pandya, 1964).…”

Heterocyclic steroids: Synthetic routes and biological characteristics of steroidal fused bicyclic pyrimidines

“…Generally, the pentacyclic pyrimidines could be obtained from the condensation of 2‐hydroxymethylene‐3‐oxo‐steroids with each of urea, thiourea, and guanidine or by treatment of ketones with tris ‐formylaminomethane, [ 40 ] and cyano‐guanidine. [ 41 ]…”

“…Gen erally, the pentacyclic pyrimidines could be obtained from the condensation of 2-hydroxymethylene-3-oxosteroids with each of urea, thiourea, and guanidine or by treatment of ketones with tris-formylaminomethane, [40] and cyano-guanidine. [41] Recently, Elattar group reviewed the chemistry of nonsteroidal bicyclic pyrimidines such as the class of pyridopyrimidines and pyrimidopyrimidines highlighting their biological applications. [42][43][44][45][46][47][48] More recently, Elattar group [49] reported the chemistry and biological applications of steroids fused to monocyclic pyrimidines and their binary analogues.…”

Στεροειδη Παραγωγα Ιμιδαζοπυριδινων

“…OH !,' CH 3 II COOH III ένω δυαμυνοπυρυμυδυνο-στεροει,δη τοϋ τύπου IV δρουν ώς μυκροβυοκτο'να (9). ΝΗ 2 IV ΝΗ 2 'Αφ*ετέρου άπλαΰ μορφαυ ΰμυδαζο(1,2-α)πυρυδυνων (V,VI) ανα φέρονται, πολλάκυς εΰζ την βι,βλυογραφιίαν ώς εχουσαυ άναλγητυκην 5 άντι,φλογυάτυκην η άντυπυρετυκην δρασυν (10,11,12) Ή 2-βρωμοχοληστανόνη παρεσκευάσθη συμφώνως προς την με'θοδον τοΰ Djerassi (14) δυο* χρήσεως ύπερβρωμυκης ύδροβρωμυκης πυρυδόνης.…”