| 摘要 |
The invention relates to derivatives of antibiotic sparsomycin A of formul/sA <FORM:1058673/C2/1> <FORM:1058673/C2/2> wherein R1 is hydrogen or alkyl and R is hydrogen, hydrocarbon carboxylic acid acyl of from 2 to 12 C atoms; halo, nitro, hydroxy, amino, cyano, thiocyano or C1- 6 alkoxy-substituted hydrocarbon carboxylic acid acyl of from 2-12 C atoms; or C1- 6 alkoxy-carbonyl. 7-D-ribofuranosyl-7H-pyrrolo-[2,3-d]-pyrimidin-4-ol (A) is prepared by reacting sparsomycin A with barium nitrite and an acid. The corresponding acylates are obtained by conventional acylation procedures, e.g. 21,31,51-triacetate; (B) by treating (A) with acetic anhydride. 7 - D - ribofuranosyl - 7H - pyrrolo-[2,3-d] pyrimidin-4-thiol 21,31,51-triacetate (C) is prepared by treating (B) with phosphorus pentasulphide; and (C) may be deacylated by treatment with methanolic sodium methoxide. The -O-alkyl and -S-alkyl compounds are obtained by alkylation of the 4-OH and 4-SH compounds. |
