Project's information

Project's title Synthesis of antidiabetic drug metformin hydrochloride for preparation of two components medicine metformin hydroclorid and glibenclamit
Research hosting institution Institute of Chemistry
Project leader’s name Associate.Professor. Nguyen Van Tuyen
Project duration 01/01/2010 - 01/01/2011
Project’s budget 400.000.000 VND
Classify Excellent
Goal and objectives of the project

Developing a procedure for the synthesis and purification of metfomin hydrochloride, used as diabetes drug in accordance with the conditions of Vietnam and pharmaceutical standards.
Main results
  • The project has synthesized directly metformin from dimethyl amine and dicyano diamide in the solvent DMF, toluene, t-BuOH and DMSO in the presence or absence of alkaline agents with different time and temperature.
  • The project has studied to synthesize metfomin hydrochloride by three different methods: direct condensation of dimethyl amine and dicyano diamide in the presence of HCl (12N), direct condensation of dimethyl amine and dicyano diamide in the presence of HCl gas; direct condensation of dicyano diamide and dimethyl amine hydrochloride. The results showed that the direct condensation of dicyano diamide and dimetylamine at 1400C for 6h giving metfomin hydrochloride with 70%  yield.
  • The project has studied the optimal and stable procedure  for  synthesis and purification metformin hydrochloride with the scale of 50g/batch. Products reached 99.8% purity.
  • 100g metformin hydrochloride has been synthesized.
  • Determined acute toxicity LD50 of metformin hydrochloride, the LD50 value = 1540mg/kg.
  • Having elaborated the basic standards of metformin hydrochloride.
Novelty and actuality and scientific meaningfulness of the results

The project has given a complete procedure to synthesize metformin hydrocloride by direct condensation of dicyano diamide and dimethyl amine with 70% yield and purification method of metformin hydrochloride. The concentration of product reached 99.8%.
Products of the project
  • Scientific papers in referred journals: 01 paper in scientific conference of the Institute of Chemistry in 2011 and 01 article is waiting for publish in Journal of Chemistry.
  • Technological products:
  1. 100g metformin hydrochloride
  2. The procedure for the synthesis and purification of metformin hydrochloride with the scale of 50g/batch
  3. The 1H-NMR, 13C-NMR, MS spectroscopic data of metformin  hydrochloride
  4. Profile of acute toxicity of metformin hydrochloride
  5. Basic standard
Research region

Results of this project will be the premise for the research of Medicinal Chemistry Programs in 2012-2013.