3 results about "Intramolecular reaction" patented technology

The present invention relates to a novel synthetic procedure utilizing domino Knoevenagel- cyclization reactions, in which the furan, thiophene or pyrrole subunits of the substrates undergo a Diels-Alder cycloaddition as either a diene or a dienophile producing novel condensed tetra- penta- or hexacycles with bridged or spirocyclic dihydrofuran, -thiophene or -pyrrole moiety. The five-membered aromatic heterocyclic subunit reacts intramolecularly as a diene with the double bond in a [4+2] or [4+4] cycloaddition (1,4-addition to five-membered heterocycle) producing bridged scaffolds. The cyclization step can also be an intramolecular hetero Diels- Alder reaction, in which a heterodiene reacts intramolecularly with the π-excessive five- membered heterocycles acting as a dienophile in the 1,2-addition. Some of the novel condensed heterocyclic products have antiproliferative activity and thus both the compounds and their therapeutic application are subject of the invention.

This invention provides a 2,3-dihydrobenzo[d][1,3]oxaphosphazene derivative of formula (I) and its preparation method. Compound I is constructed by tandem nucleophilic addition (or nucleophilic substitution) and intramolecular S-NAr reaction. This method features simple preparation steps, high yield, and mild reaction conditions, solving the technical problems of complex synthesis steps and harsh conditions in the synthesis of oxaphosphine compounds in traditional prior art.

The invention provides a preparation method of an AT-406 intermediate, and belongs to the technical field of medical intermediates. According to the method, methyl L-pyroglutamate is subjected to ethynylation, and a selected ester solvent and a hydroboration reagent are subjected to hydroboration reductive amination reaction, so that the reaction selectivity can be improved, isomer impurities are reduced, separation and purification are easy, a single cis-configuration product can be obtained, and the ee value can reach 99.5% or above. The specific hydroboration reagent and the oxidation reagent are selected, so that the use of ozone and reagents with strong mercaptan odor is avoided, the selectivity of intramolecular reaction is improved, the generation of byproducts is reduced, separation and purification are easy, the catalyst and the byproducts are non-toxic and pollution-free to the environment, and the method is suitable for industrial production. The invention provides a method suitable for industrial production to obtain the AT-406 intermediate.