LM-1554

合成路线:LM-1554 is synthesized by condensation of 2-amino-3-carbethoxy-4,5,6,7-tetrahydrobenzo[b]thiophene (I) with chloroacetonitrile (III) in the presence of dry hydrogen chloride gas followed by basification.Alternatively,2-amino-3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophene (IV) can be condensed with chloroacetonitrile (III) under the above reaction conditions.The condensation of (I) with chloroacetamide (II) in the presence of an equivalent of phosphorus oxychloride in chloroform followed by basification also yields LM-1554.

合成路线:By reaction of 2-aminobenzophenones (I) with bromoacetyl halide (II) or tosyloxyacetyl halide (VI) to give,respectively,2-(bromoacetylamino)benzophenones (III) or 2-(tosyloxyacetylamino)benzophenones (VII),which are treated with ethanolamine (IV) to give the compounds (V),which with acetic acid in ethanol give the desired compounds.These compounds can also be obtained from (III) and (VI) without isolation of (V)
参考文献标题:Process for the manufacture of pharmacologically active new heterocyclic compounds and salts thereof
文献作者:Shishoo,C.J.; et al.
参考来源:IN 151496