A kind of synthesis method of medicine for treating leukemia

Abstract

The invention relates to a synthesis method of a drug for treating leukemia. The synthesis method comprises that 1, a compound 3-methyl-3-oxetanemethanol and sodium metal undergo a reaction to produce 3-sodium methoxide-3-methyl-3-oxetane, 2, 4-amino-3-nitrochlorobenzene is added into the product obtained by the step 1 so that reddish-orange solids (A1) are obtained, a compound 8-benzyloxyquinolin-2-chlorine and A1 undergo a reaction to produce orange solids A2, 3, the compounds A2, 13g of palladium / carbon and formic acid undergo a reaction, formamidine acetate is added into the reaction product, and the mixture is subjected to reflux and drying so that white-like (or yellow) solids A3 are obtained, and 4, the compounds A3 and benzenesulfonyl chloride undergo a reaction, the product is dried to form maize-yellow solids A4, BINAP, A4, tert-butyl piperidin-4-yl-carbamate and potassium carbonate undergo a reaction, the reaction product is dried to form A5, and the A5 is refined through the step 5 so that a pure product is obtained. In the steps 1 and 2, a one-pot method is used.

Description

Technical field: [0001] The invention relates to the preparation of pharmaceutical compounds, in particular to a synthesis method of anticancer drugs. Background technique: [0002] Acute myeloid leukemia (AML) is a type of hematological malignancy with highly heterogeneous genetics. By detecting chromosomal abnormalities and gene mutations, the disease can be used for risk classification and prognosis assessment. The current international standard treatment regimen includes induction therapy containing cytarabine and anthracyclines, followed by consolidation therapy and hematopoietic stem cell transplantation. Although high-dose chemotherapy can benefit patients in the short term, most patients may experience disease recurrence, and whether the disease relapses or is refractory, the effect of subsequent high-dose chemotherapy is often unsatisfactory, and the options for treatment strategies are also very limited. , leading to a poor prognosis. Therefore, how to treat rela...

AI Technical Summary

Problems solved by technology

[0011] The above route involves some unusual and expensive reagents such as: N-phenyl-bis(trifluoromethanesulfonimide), tris(dibenzylideneacetone)dipalladium, 4,5-bis(diphenyl base)-9,9-dimethyltricyclic dibenzo ligand (Xantphos), etc., in addition to flammable and explosive sodium hydride and toxic, corrosive, explosive and poisonous boron tribromide, etc. etc., and mixed solvents are used, it is not easy to recycle, and it is easy to cause unnecessary pollution to the environment. These factors are not suitable for industrial production

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