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An Improved Synthesis of Finasteride from 4-Androsten-3,17-Dione


Affiliations
1 Department of Pharmaceutical Chemistry and Center for New Drugs Discovery and Development (C3D), Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem District, Hanoi, Viet Nam
     

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An improved synthesis of 3-oxo-4-aza-5α-androst-1-ene-17β-(N-tert-butylcarboxamide), commonly known as finasteride (1), a drug widely used for the treatment of benign prostatic hyperplasia (BPH), has been implemented via seven steps in an overall yield of 20.01% starting from 4-androsten-3,17-dione (AD). Conditions of several steps have been improved to be less expensive and more commercially viable compared to reported synthesis in literature.

Keywords

Finasteride, Benign Prostatic Hyperplasia, Androst-4-En-3,17-Dione, Synthesis.
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  • An Improved Synthesis of Finasteride from 4-Androsten-3,17-Dione

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Authors

Nguyen Hai Nam
Department of Pharmaceutical Chemistry and Center for New Drugs Discovery and Development (C3D), Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem District, Hanoi, Viet Nam
Ngo Anh Ngoc
Department of Pharmaceutical Chemistry and Center for New Drugs Discovery and Development (C3D), Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan Kiem District, Hanoi, Viet Nam

Abstract


An improved synthesis of 3-oxo-4-aza-5α-androst-1-ene-17β-(N-tert-butylcarboxamide), commonly known as finasteride (1), a drug widely used for the treatment of benign prostatic hyperplasia (BPH), has been implemented via seven steps in an overall yield of 20.01% starting from 4-androsten-3,17-dione (AD). Conditions of several steps have been improved to be less expensive and more commercially viable compared to reported synthesis in literature.

Keywords


Finasteride, Benign Prostatic Hyperplasia, Androst-4-En-3,17-Dione, Synthesis.