Laboratory Synthesis Of Acyclovir

Chemical Name IUPAC : 2- amino- 1 ,9- di hydro- 9- [(2- hydroxy ethoxy )methyl]- 6 H- purin- 6- one

Acyclovir Use: antiviral

Acyclovir MW: 225.21

Acyclovir MF: C8H11N5O3

Acyclovir LD50: 1000 mg/kg (M, i.p.); 1118 mg/kg (M, i.v.); >10000 mg/kg (M, p.o.); 1118 mg/kg (M,s.c.);860 mg/kg (R, i.p.); 910 mg/kg (R, i.v.); >20000 mg/kg (R, p.o.); 620 mg/kg (R, s.c.)

Reference(s):

1. Schaeffer, H.J. et al.: Nature (London) (NATUAS) 272, 583 (1978).
2. DE 2 539 963 (Wellcome; appl. 2.9.1975; GB-prior. 2.9.1974).
3. US 4 199 574 (Wellcome; 22.4.1980; GB-prior. 2.9.1974).
4. c GB 1 567 671 (Wellcome; appl. 26.8.1977; USA-prior. 27.8.1976).
5. Matsumoto, H. et al.: Chem. Pharm. Bull. (CPBTAL) 36, 1153 (1988).
6. f EP 709 385 (Roche; appl. 13.7.1995; USA-prior. 26.7.1994, 27.4.1995).

Aternative synthesis Acyclovir from 4-aminoimidazole-5-carboxamide:

WO 9 011 283 (GEA Farm.; 4.10.1990; DK-prior. 20.3.1989).

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