FIELD: chemistry.
SUBSTANCE: invention relates to an improved method of producing N-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-5-pyrimidine-sulphone)-N'-isonictinoyl hydrazide used as substance for medicinal agents for treating and preventing immunodeficiency during infectious and somatic pathology ('Isofon'), treating mycobacterial and viral infections ('Tubosan'). The method involves reaction of 6-methyluracil-5-sulphochloride with isonicotinic acid hydrazide in equimolar amounts in the medium of a mixture of ethyl acetate and alcohol - ethyl or isopropyl or methyl alcohol, taken in ratio 95-90:5-10 vol. % at temperature 40-73°C for not less than two hours, followed by distillation of the solvent from the reaction mass, dissolution and purification of the reaction product in aqueous ammonia solution and neutralisation of the purified solution to pH not higher than 5. All steps of the process of producing the end product are carried out in a single cycle without extracting intermediate products.
EFFECT: method enables to reduce the cost of raw materials, avoid loss of the end product during intermediate operations, increase output of a pharmaceutically pure agent, cut the duration of the process and reduce labour input.
6 ex
Title | Year | Author | Number |
---|---|---|---|
METHOD OF PRODUCING N-(6-METHYL-2,4-DIOXO-1,2,3,4-TETRAHYDRO-5-PYRIMIDINE-SULPHONE)-N'-ISONICOTINOYL HYDRAZIDE | 2011 |
|
RU2458059C1 |
METHOD OF OBTAINING AND PURIFYING N-(6-METHYL-2,4-DIOXO-1,2,3,4-TETRAHYDRO-5-PYRIMIDINE-SULPHONE)-N'-ISONICTINOYL HYDRAZIDE | 2009 |
|
RU2404977C1 |
METHOD FOR PREPARING N-(6-METHYL-2,4-DIOXO-1,2,3,4-TETRAHYDRO-5-PYRIMIDINSULFON)-N'-ISONICOTINO YL HYDRAZIDE | 2003 |
|
RU2235723C1 |
IMMUNOMODULATING AGENT "IZOFON" SHOWING ANTIMYCOBACTERIAL ACTIVITY, METHOD OF ITS PREPARING AND USING | 1997 |
|
RU2141322C1 |
SILVER SALT OF N-(6-METHYL-2,4-DIOXO-1,2,3,4-TETRAHYDRO-5H-PYRIMIDINESULPHONE)-N'-ISONICOTINOYLHYDRAZIDE, WHICH EXHIBITS IMMUNOTROPIC, ANTIMICROBIAL, ANTIFUNGAL (ANTIMYCOTIC) ACTIVITY AND MEDICINAL AGENT BASED ON SAID SALT | 2008 |
|
RU2368609C1 |
6-ALKYL-5-(2-ISONICOTINOYLSULFOHYDRAZOYL)URACIL HYDROCHLORIDE AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF | 2003 |
|
RU2264396C2 |
N-(6-METHYL-2,4-DIOXO-1,2,3,4-TETRAHYDRO-5H-PYRIMIDINESULFONE)-N′- ISONICOTINOYL HYDRAZIDE DISODIUM SALT ELICITING ANTIBACTERIAL AND IMMUNOTROPIC ACTIVITY AND MEDICINAL AGENT BASED ON THEREOF | 1999 |
|
RU2191015C2 |
CITRACONIC ACID ISONICOTINOYLHYDRAZIDE ELICITING HYPOGLYCAEMIC ACTIVITY | 2000 |
|
RU2183625C2 |
PHTHALIC ACID ISONICOTINOYL HYDRAZIDE ELICITING HYPOGLYCEMIC ACTIVITY | 2002 |
|
RU2228753C2 |
MEDICINAL AGENT | 2002 |
|
RU2223100C1 |
Authors
Dates
2012-07-10—Published
2010-08-06—Filed