產(chǎn)品名稱: |
N-2-乙酰更昔洛韋 |
化學(xué)名: |
N-(9-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]-6-oxo-6,9-dihydro-1H-purin-2-yl)acetamide |
CAS#: |
84245-12-5 |
分子式: |
C11H15N5O5 |
分子量: |
297.2727 |
含量: |
>98.0% |
外觀: |
類白色粉末 |
分子式: |
|
9-(1,3-Dihydroxy-2-propoxymethyl)guanine as antiviral agent
100:126895 9-(1,3-Dihydroxy-2-propoxymethyl)guanine as antiviral agent. Verheyden, Julien P. H.Some chemicals with cas registry numbers like 84245-11-4 and 84245-12-5 are also used.; Martin, John C. (Syntex (U.S.A.), Inc., USA). U.S. US 4423050 A 27 Dec 1983, 6 pp. Cont.-in-part of U.S. 4,355,032. (English). (United States of America). CODEN: USXXAM. CLASS: IC: A61K031-52. NCL: 424253000. APPLICATION: US 82-380969 24 May 1982. PRIORITY: US 81-267210 21 May 1981. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1, 28 9-(1,3-Dihydroxy-2-propoxymethyl)guanine (I) [82410-32-0] is effective in treating viral infections. 1,3-Di-O-benzylglycerol [6972-79-8] was prepd. by the addn. of epichlorohydrin [106-89-8] to benzyl alc. [100-51-6] in the presence of NaH in DMF at 15-40°. The dibenzylglycerol was chloromethylated with HCl and paraformaldehyde, and the 1,3-di-O-benzyl-2-O-chloromethylglycerol [74564-16-2] was treated with NaOAc [127-09-3] at 0° to give 2-O-acetoxymethyl-1,3-di-O-benzylglycerol [84245-11-4]. The latter was condensed with N2,9-diacetylguanine [3056-33-5], formed by the acetylation of guanine [73-40-5]. The protective benzyl groups were removed from the N2-acetyl-9(1,3-dibenzyloxy-2-propoxymethyl)guanine [82410-30-8] by catalytic hydrogenation. The N2-acetyl-9-(1,3-dihydroxy-2-propoxymethyl)guanine [84245-12-5] was deacetylated with NH3-satd. MeOH at 0° to give I. I Na salt [84245-13-6] could be prepd. with aq. NaOH. The formulation of topical, i.p., i.m,., and i.v. injections, and tablets is described. Administration of 10 mg I/kg s.c. 6, 24, 48, 72, and 96 h to mice with herpes simplex 2 virus after i.p. injection of 10 LD50 of the virus gave 19, 18, and 18 survivors of 20, 12, 14, and 21 days after virus challenge vs. 0 for the controls. . |