Synthesis of 6-amino-4-methyl-8-(.beta.-D-ribofuranosyl)pyrrolo[

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 28, 536 26, 536 27, 536 24, 536 23, 536 29, A61K 3170, C07H 1902

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041235240

ABSTRACT:
The compound 6-amino-4-methyl-8-(.beta.-D-ribofuranosyl)pyrrolo[4,3,2-de]pyrimido[4,5-c ]pyridazines-5'-phosphate (a nucleotide) as a new compound and its method of synthesis by phosphorylation of the known 6-amino-4-methyl-8-(.beta.-D-ribofuranosyl)pyrrolo[4,3,2-de]pyrimido[4,5-c ]pyridazine (a nucleoside). The 5'-phosphate ester has utility against L-1210 mouse leukemia and has superior solubility over the parent compound which gives it a broader use pattern relative to dosage. This novel nucleotide also shows advantage in utilization as to pH over, for example, the hydrochloride salt which gives in solution a pH of 4 and is too acid for use.

REFERENCES:
patent: 3413282 (1968-11-01), Yoshikawa et al.
Towsend, L. and Schram, K., Tetrahedron Letter, 1971, No. 49, pp. 4757-4760.

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