| 摘要 |
FIELD: organic chemistry, chemical technology, biochemistry, pharmacy. ^ SUBSTANCE: invention relates to effective and economy methods for preparing intermediate compounds used for synthesis of inhibitors of HIV-protease that are related to nelfinavir-mesylate and comprising nelfinavir-mesylate. Invention relates to a method for preparing oxazoline wherein substitute Rb represents hydrogen atom, -COR(3), -SO2R(2) or suitable hydroxyl-protecting group; substitute RC represents hydrogen atom, -COR(3) or -SO2R(2) wherein R(1), R(2) and R(3) represent independently of one another substituted or unsubstituted alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl group: ^ from tetrahydrofuran wherein substitute Ra represents -COR(1); substitute Rb represents hydrogen atom, -COR(3), -SO2R(2) or suitable hydroxyl-protecting group: ^ . Method involves treatment of tetrahydrofuran with oxophilic electrophilic reagent by method that gives oxazoline effectively. Also, invention describes preparing key reactive intermediate compounds used for synthesis of nelfinavir. ^ EFFECT: improved preparing method. ^ 30 cl, 5 ex |
