| 摘要 |
1363064 Pyrimidines and pteridines WELLCOME FOUNDATION Ltd 13 July 1971 [27 July 1970] 36289/70 Heading C2C Novel compounds of the Formula IV wherein Z is C 1-4 alkyl optionally having a methylene group attached to the ring system or hydroxymethyl may be prepared by condensing a 2 - amino - 4 - halogeno - 6 - hydroxy - 5- nitropyrimidine with a compound V The compounds IV may be reductively cyclized, optionally via the free ketone of IV, to a pteridine compound II Compounds of the Formula V may be prepared either by treatment of compound VII wherein X is Z or when Z is CH 2 OH an alkyl ester thereof, with isoamyl nitrite and hydrochloric acid to yield the compound VI followed by treatment of VI with ammonia to yield V, or forming the oxime of 3-amino-3- methyl butan-2-one. The intermediate VI may be formed by reduction of 1,1-dimethylacrylic acid (X = CH 2 OH), optionally followed by esterification (X = CH 2 O.COR), (R=alkyl) or re-arrangement of 3-methyl-3-hydroxy-but.-1-ene. 3 - Amino - 2 - methyl - butan - 2 - one may be prepared by condensation of 2-nitropropane and acetaldehyde in the presence of base to yield 3-nitro-3-methyl butan-2-ol which is reduced to 3-amino-3-methyl butan-2-ol acylated with benzoyl chloride to 3-N-benzoylamino-3- methyl butan-2-ol which is oxidized to 3-N- benzoylamino-3-methyl butan-2-one which is hydrolysed to the required product. Pharmaceutical compositions of the compounds II in which Z is C 1-4 alkyl show antibacterial activity when administered parenterally or orally with the usual excipients. |
