| 摘要 |
NEW MATERIAL:The compound of formulaI(R<1> is halogen; R<2> is H or halogen; R<3> is methyl, ethyl, or hydroxyethyl). EXAMPLE:1-(4-Chlorophenylthio)-2-methylaminopropane fumarate. USE:Preventive and remedy for obesity and diabetes. It has low toxicity and is free from stimulating action to central vervous system. It can be administered safely for a long period. PROCESS:The compound of formulaIis prepared by reacting the thiophenol derivative of formula II with chloroacetone according to the reaction formula, and subjecting the resultant compound of formula III to the reductive amination reaction with R<3>NH2 using LiBH3CN or NaBH3CN as a reducing agent. The reaction is carried out in a solvent such as methanol, in the presence of 1-3mol of an acid such as HCl, using 2-20mol of R<3>NH2 based on 1mol of the compound of formula III. |
