| 摘要 |
Hydroxy alkyl purines I (R=OH; R1=C1-8 alkyl) were prepd. Thus, Me(CH2)5CH(NH2)COOH was treated with Ac2O in the presence of pyridine to give 70% Me(CH2)5CH(NH2)COMe, which was quaternized and reduced with KBH4 to give 75% Me(CH2)5CH(NH2)CHMeOH. The alkanolamine was condensed with 5-amino-4,6-dichloro pyrimidine to give 54% of the pyrimidinediamine, which was cyclized with HC(OEt)3 to give *≮R = Cl, R1 - (CH2-)5Me≉ quant. The chloropurine was quant. hydrolyzed to I ≮R = OH, R1 = (CH2)5Me≉ which, had immune adjuvant activity in mice at 10 mg/kg orally.
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