METHOD FOR SYNTHESIS OF 3β-HYDROXY-17-(1H-BENZIMIDAZOL-1-YL)ANDROSTA-5,16-DIENE Russian patent published in 2021 - IPC C07J43/00 C07J75/00 

Abstract RU 2749134 C1

FIELD: organic chemistry.

SUBSTANCE: invention relates to the field of organic chemistry, namely to a method for synthesis of 3β-hydroxy-17-(1H-benzimidazol-1-yl)androst-5,16-diene (6) (galeterone), including an interaction between 17-iodandrost-5,16-diene-3β-ol (I) and benzimidazole in the presence of an organic solvent, a base, copper iodide and 8-hydroxyquinoline, wherein 8-hydroxyquinoline is used in an amount of no less than 1.8% wt. relative to the compound (I), and copper iodide (CuI) is used in an amount of 1.2% wt. to 5% wt. relative to the compound (I) used in the reaction, wherein the reaction temperature is between 130°C and 200°C. The invention also relates to an intermediate compound 3β-hydroxy-17-(1H-benzimidazol-1-yl) androst-5,16-diene dioxalate (galeterone).

EFFECT: new method for synthesis of galeterone is developed characterized by simplicity and easy implementation in industry.

15 cl, 3 dwg, 10 ex

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RU 2 749 134 C1

Authors

Barbieri, Francesco

Lenna, Roberto

Dates

2021-06-04Published

2017-08-08Filed