A PROCESS FOR SYNTHESIS OF HETEROCYCLIC AMINOALKYL BENZAMIDES

摘要

The simple, new, original and convenient for use, procedure for obtaining of compounds, belonging to the group of $i(heterocyclic aminoalkyl benzamides) of general formula 1, is developed, and/or salts and/or hydrates and/or optical isomers thereof, wherein R1 and R2 denote C1-C4 $i(alkyl) group, R3 denotes an $i(aminosulphonyl) group, denotes a $i(hydrogen) atom or an $i(amino) group, R5 denotes a $i(hydrogen) or a $i(halogen) atom, and and the coefficients $i(m )and $i(n) have value of 1 and/or 2. Of a particular interest in clinical practice are: $i(sulpiride )(RS, R+ or S-)-(5-$i(aminosulphonyl))-N-/(1-$i(ethyl)-2-$i(pyrrolidinyl))$i(methyl)/-2-$i(methoxybenzamide)) and sulmepride (RS, R+ or S-)-(5-($i(aminosulphonyl))-2-$i(methoxy)-N-/-(1-$i(methyl-)2-$i(pyrrolidinyl)methyl/benzamide)). The compounds belonging to this group are used in therapy as: antipsychotics, anti depressives and anti emetics, fungicides, for contraceptive mixtures, in treatment of sterility, as radiopharmaceutical compositions in nuclear medicine, in treatment of migraine of various origins, as well as in treatment of parkinsonism. The advantage of the present invention is in its completely new and simple way to carry out the synthesis of $i(heterocyclic aminoalkyl benzamides )and/or salts and/or hydrates thereof, through reaction of $i(2-alcoxy-5-suiphamoyl-alkyl benzoate )with the corresponding (RS R+ or S-) heterocyclic amine. )Lower temperature of rection and work at atmospheric pressure without catalysts, performing the reaction in cheaper and safer organic solvents, i obtaining the final product which does not require any additional purification, achieving of I good yield and high quality of the final product, cheaper procedure for industrial use and obtaining of the product of high pharmacopeic purity.