阿昔洛韦 [CAS59277893]详细合成路线原料药厂家武汉东康源.docVIP

药物详细合成路线 Name Acycloguanosine;Aciclovir;Acyclovir;W-248-U;BW-248-U;Maynar;Viropump(former Brand Name);Genvir;Zovirax Chemical Name 9-(2-Hydroxyethoxymethyl)guanine;2-Amino-6-hydroxy-9-(2-hydroxyethoxymethyl)purine;2-Amino-9-[(2-hydroxyethoxy)methyl]-1,9-dihydro-6H-purin-6-one CAS 59277-89-3 Related CAS Formula C8H11N5O3 Structure Formula Weight 225.20857 Stage 上市-1981 Company Activity/Mechanism Anti-Herpes Labialis Drugs, Anti-Herpes Simplex Virus Drugs, Anti-Herpes Virus Drugs, ANTIINFECTIVE THERAPY, Anti-Varicella Zoster Virus Drugs, Antiviral Drugs, Antiviral Ophthalmic Drugs, Ocular Antiinflammatory and Antiinfective Agents, OCULAR MEDICATIONS, Ophthalmic Drugs tel 86-027mail chem@ Syn. Route 4 Route 1 an efficient and selective process for the synthesis of acyclovir has been published:the reaction of guanine (i) with refluxing hexamethyldisilazane (hmds) (ii) by means of trifluoromethanesulfonic acid, elimination of the hmds in excess and condensation of the resulting product with refluxing 1,3-dioxolane (iii) gives 9-[2-(trimethylsilyloxy)ethoxymethyl]guanine (iv), which is finally hydrolyzed with refluxing acetic acid/water. List of intermediates No. n,n-dipropylamine; n-propyl-1-propanamine (i) 1,2-di(2-oxiranyl)-1,2-ethanediol (iii) (7r)-3-[(acetoxy)methyl]-7-[[2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(methoxyimino)acetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (iv) Reference 1: han, y.-k.; harrington, p.j.; schloemer, g.c. (f. hoffmann-la roche ag); preparation of acyclovir. ep 0709385; jp 1996053451 . Route 2 the reaction of benzonitrile (i) with refluxing ethylene glycol (ii) gives ethylene glycol monobenzoate (iii), which is chloromethylated with formaldehyde and dry hcl in ch2cl2 affording 1-benzoyloxy-2-chloromethoxyethane (iv). the condensation of (iv) with 2,6-dichloropurine (v) by means of triethylamine in dmf yields 2,6-dichloro-9-(2-benzoyloxyethoxymethyl)purine (vi