| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: invention relates to a method of producing a monohydrate of (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide through contact of a compound of formula ^ ^ with aqueous methylamine at temperature equal to approximately 2.5-7.5C. The invention also relates to a method of producing an intermediate compound of formula (4): involving reaction of a compound of formula (1) with 14.3-16.7-fold molar excess hydrazine hydrate at temperature equal to approximately 60-65C to obtain the corresponding hydrazine of formula (2), followed by contact between the compound of formula (2) and excess ethyl-2-formyl-3-oxopropionate, optionally in the presence of an acid. ^ EFFECT: method enables to obtain, in a single step, a crystalline compound in form of a monohydrate and also exclude undesirable impurities of the compound of formula 2 in the end product owing to use of intermediate product 4. ^ 15 cl, 7 ex, 5 dwg |
